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Dale Boger

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Katerina Otrubova; Raymond C Stevens; Monica Brown; Benjamin F Cravatt; Gye W Han; Aron H Lichtman; Michael S McCormick; Scott T O'Neal; Dale L Boger
Rational design of Fatty Acid amide hydrolase inhibitors that act by covalently bonding to two active site residues.
Travis C Turner; Kotaro Shibayama; Dale L Boger
Hypervalent iodine(III)-promoted intermolecular C-C coupling of vindoline with β-ketoesters and related substrates.
Jian Xie; Amanda L Wolfe; Dale L Boger
Total synthesis of kopsinine.

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All Publications

2013: Katerina Otrubova; Raymond C Stevens; Monica Brown; Benjamin F Cravatt; Gye W Han; Aron H Lichtman; Michael S McCormick; Scott T O'Neal; Dale L Boger
Rational design of Fatty Acid amide hydrolase inhibitors that act by covalently bonding to two active site residues.
Journal of the American Chemical Society 2013;135(16):6289-99.
2013: Travis C Turner; Kotaro Shibayama; Dale L Boger
Hypervalent iodine(III)-promoted intermolecular C-C coupling of vindoline with β-ketoesters and related substrates.
Organic letters 2013;15(5):1100-3.
2013: Jian Xie; Amanda L Wolfe; Dale L Boger
Total synthesis of kopsinine.
Organic letters 2013;15(4):868-70.
2013: Erick K Leggans; Kristin D Schleicher; Timothy J Barker; Katharine K Duncan; Dale L Boger
A remarkable series of vinblastine analogues displaying enhanced activity and an unprecedented tubulin binding steric tolerance: C20' urea derivatives.
Journal of medicinal chemistry 2013;56(3):628-39.
2013: Steven P Breazzano; Yam B Poudel; Dale L Boger
A Pd(0)-mediated indole (macro)cyclization reaction.
Journal of the American Chemical Society 2013;135(4):1600-6.
2013: Kristin D Schleicher; Annie Tam; Katharine K Duncan; Daisuke Kato; Yoshikazu Sasaki; Dale L Boger
Total synthesis and evaluation of vinblastine analogues containing systematic deep-seated modifications in the vindoline subunit ring system: core redesign.
Journal of medicinal chemistry 2013;56(2):483-95.
2012: Landon R Whitby; Dale L Boger
Comprehensive peptidomimetic libraries targeting protein-protein interactions.
Accounts of chemical research 2012;45(10):1698-709.
2012: Timothy J Barker; Dale L Boger
Fe(III)/NaBH4-mediated free radical hydrofluorination of unactivated alkenes.
Journal of the American Chemical Society 2012;134(33):13588-91.
2012: Hiroaki Gotoh; Justin E Sears; Albert Eschenmoser; Dale L Boger
New insights into the mechanism and an expanded scope of the Fe(III)-mediated vinblastine coupling reaction.
Journal of the American Chemical Society 2012;134(32):13240-3.
2012: Amanda L Wolfe; Katharine K Duncan; Nikhil K Parelkar; George A Vielhauer; Scott J Weir; Dale L Boger
A novel, unusually efficacious duocarmycin carbamate prodrug that releases no residual byproduct.
Journal of medicinal chemistry 2012;55(12):5878-86.
2012: Akinori Okano; Joshua G Pierce; Jian Xie; Robert C James; Dale L Boger
Silver(I)-promoted conversion of thioamides to amidines: divergent synthesis of a key series of vancomycin aglycon residue 4 amidines that clarify binding behavior to model ligands.
Journal of the American Chemical Society 2012;134(21):8790-3.
2012: Robert C James; Akinori Okano; Joshua G Pierce; Jian Xie; Dale L Boger
Redesign of glycopeptide antibiotics: back to the future.
ACS chemical biology 2012;7(5):797-804.
2012: James P Lajiness; Wanlong Jiang; Dale L Boger
Divergent total syntheses of (-)-aspidospermine and (+)-spegazzinine.
Organic letters 2012;14(8):2078-81.
2012: Landon R Whitby; Xiaoqian Yu; Kristopher E Boyle; Lifeng Cai; Miriam Gochin; Dale L Boger
Discovery of HIV fusion inhibitors targeting gp41 using a comprehensive α-helix mimetic library.
Bioorganic & medicinal chemistry letters 2012;22(8):2861-5.
2012: Lamont Booker; Benjamin F Cravatt; Cyrine Ezzili; Steven G Kinsey; Rehab A Abdullah; Jacqueline L Blankman; Dale L Boger; Jonathan Z Long; Aron H Lichtman
The fatty acid amide hydrolase (FAAH) inhibitor PF-3845 acts in the nervous system to reverse LPS-induced tactile allodynia in mice.
British journal of pharmacology 2012;165(8):2485-96.
2012: Erick K Leggans; Katharine K Duncan; Timothy J Barker; Dale L Boger
Iron(III)/NaBH4-mediated additions to unactivated alkenes: synthesis of novel 20'-vinblastine analogues.
Organic letters 2012;14(6):1428-31.
2012: Jian Xie; Christine M Crane; Robert C James; Akinori Okano; Joshua G Pierce; Simon Stamm; Dale L Boger
Total synthesis of [Ψ[C(═S)NH]Tpg4]vancomycin aglycon, [Ψ[C(═NH)NH]Tpg4]vancomycin aglycon, and related key compounds: reengineering vancomycin for dual D-Ala-D-Ala and D-Ala-D-Lac binding.
Journal of the American Chemical Society 2012;134(2):1284-97.
2011: Steven P Breazzano; Dale L Boger
Synthesis and stereochemical determination of complestatin A and B (neuroprotectin A and B).
Journal of the American Chemical Society 2011;133(45):18495-502.
2011: Jian Xie; Robert C James; Akinori Okano; Joshua G Pierce; Dale L Boger
A redesigned vancomycin engineered for dual D-Ala-D-ala And D-Ala-D-Lac binding exhibits potent antimicrobial activity against vancomycin-resistant bacteria.
Journal of the American Chemical Society 2011;133(35):13946-9.
2011: Katerina Otrubova; Cyrine Ezzili; Dale L Boger
The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH).
Bioorganic & medicinal chemistry letters 2011;21(16):4674-85.
2011: Erin D Anderson; Dale L Boger
Inverse electron demand Diels-Alder reactions of 1,2,3-triazines: pronounced substituent effects on reactivity and cycloaddition scope.
Journal of the American Chemical Society 2011;133(31):12285-92.
2011: Landon R Whitby; Yoshio Ando; Bryan L Roth; Vincent Setola; Peter K Vogt; Dale L Boger
Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions.
Journal of the American Chemical Society 2011;133(26):10184-94.
2011: Erin D Anderson; Dale L Boger
Scope of the inverse electron demand Diels-Alder reactions of 1,2,3-triazine.
Organic letters 2011;13(9):2492-4.
2011: Cyrine Ezzili; Mauro Mileni; Nicholas McGlinchey; Jonathan Z Long; Steven G Kinsey; Dustin G Hochstatter; Raymond C Stevens; Aron H Lichtman; Benjamin F Cravatt; Edward J Bilsky; Dale L Boger
Reversible competitive α-ketoheterocycle inhibitors of fatty acid amide hydrolase containing additional conformational constraints in the acyl side chain: orally active, long-acting analgesics.
Journal of medicinal chemistry 2011;54(8):2805-22.
2011: Mauro Mileni; Joie Garfunkle; Cyrine Ezzili; Benjamin F Cravatt; Raymond C Stevens; Dale L Boger
Fluoride-mediated capture of a noncovalent bound state of a reversible covalent enzyme inhibitor: X-ray crystallographic analysis of an exceptionally potent α-ketoheterocycle inhibitor of fatty acid amide hydrolase.
Journal of the American Chemical Society 2011;133(11):4092-100.
2011: James P Lajiness; Dale L Boger
Asymmetric synthesis of 1,2,9,9a-tetrahydrocyclopropa[c]benzo[e]indol-4-one (CBI).
The Journal of organic chemistry 2011;76(2):583-7.
2010: Annie Tam; Hiroaki Gotoh; William M Robertson; Dale L Boger
Catharanthine C16 substituent effects on the biomimetic coupling with vindoline: preparation and evaluation of a key series of vinblastine analogues.
Bioorganic & medicinal chemistry letters 2010;20(22):6408-10.
2010: James P Lajiness; William M Robertson; Irene Dunwiddie; Melinda A Broward; George A Vielhauer; Scott J Weir; Dale L Boger
Design, synthesis, and evaluation of duocarmycin O-amino phenol prodrugs subject to tunable reductive activation.
Journal of medicinal chemistry 2010;53(21):7731-8.
2010: Géza Ambrus; Landon R Whitby; Eric L Singer; Oleg Trott; Euna Choi; Arthur J Olson; Dale L Boger; Larry Gerace
Small molecule peptidomimetic inhibitors of importin α/β mediated nuclear transport.
Bioorganic & medicinal chemistry 2010;18(21):7611-20.
2010: Cyrine Ezzili; Katerina Otrubova; Dale L Boger
Fatty acid amide signaling molecules.
Bioorganic & medicinal chemistry letters 2010;20(20):5959-68.
2010: Christine M Crane; Joshua G Pierce; Siegfried S F Leung; Julian Tirado-Rives; William L Jorgensen; Dale L Boger
Synthesis and evaluation of selected key methyl ether derivatives of vancomycin aglycon.
Journal of medicinal chemistry 2010;53(19):7229-35.
2010: James P Lajiness; Dale L Boger
Synthesis and characterization of a cyclobutane duocarmycin derivative incorporating the 1,2,10,11-tetrahydro-9H-cyclobuta[c]benzo[e]indol-4-one (CbBI) alkylation subunit.
Journal of the American Chemical Society 2010;132(39):13936-40.
2010: Yoshikazu Sasaki; Daisuke Kato; Dale L Boger
Asymmetric total synthesis of vindorosine, vindoline, and key vinblastine analogues.
Journal of the American Chemical Society 2010;132(38):13533-44.
2010: Paresma R Patel; Dale L Boger
Intramolecular Diels-Alder reactions of cyclopropenone ketals.
Organic letters 2010;12(15):3540-3.
2010: Max W Chang; Michael J Giffin; Rolf Muller; Jeremiah Savage; Ying C Lin; Sukwon Hong; Wei Jin; Landon R Whitby; John H Elder; Dale L Boger; Bruce E Torbett
Identification of broad-based HIV-1 protease inhibitors from combinatorial libraries.
The Biochemical journal 2010;429(3):527-32.
2010: Paresma R Patel; Dale L Boger
Intramolecular [1 + 2] and [3 + 2] cycloaddition reactions of cyclopropenone ketals.
Journal of the American Chemical Society 2010;132(25):8527-9.
2010: Porino Va; Erica L Campbell; William M Robertson; Dale L Boger
Total synthesis and evaluation of a key series of C5-substituted vinblastine derivatives.
Journal of the American Chemical Society 2010;132(24):8489-95.
2010: Hiroyuki Shimamura; Steven P Breazzano; Joie Garfunkle; F Scott Kimball; John D Trzupek; Dale L Boger
Total synthesis of complestatin: development of a Pd(0)-mediated indole annulation for macrocyclization.
Journal of the American Chemical Society 2010;132(22):7776-83.
2010: William M Robertson; David B Kastrinsky; Inkyu Hwang; Dale L Boger
Synthesis and evaluation of a series of C5'-substituted duocarmycin SA analogs.
Bioorganic & medicinal chemistry letters 2010;20(9):2722-5.
2010: Daisuke Kato; Yoshikazu Sasaki; Dale L Boger
Asymmetric total synthesis of vindoline.
Journal of the American Chemical Society 2010;132(11):3685-7.
2010: Kristopher E Boyle; Karen S MacMillan; David A Ellis; James P Lajiness; William M Robertson; Dale L Boger
Synthesis and evaluation of duocarmycin SA analogs incorporating the methyl 1,2,8,8a-tetrahydrocyclopropa[c]oxazolo[2,3-e]indol-4-one-6-carboxylate (COI) alkylation subunit.
Bioorganic & medicinal chemistry letters 2010;20(6):1854-7.
2010: Erica L Campbell; Andrea M Zuhl; Christopher M Liu; Dale L Boger
Total synthesis of (+)-fendleridine (aspidoalbidine) and (+)-1-acetylaspidoalbidine.
Journal of the American Chemical Society 2010;132(9):3009-12.
2010: James S Oakdale; Dale L Boger
Total synthesis of lycogarubin C and lycogalic acid.
Organic letters 2010;12(5):1132-4.
2010: Christopher P Burke; Nadia Haq; Dale L Boger
Total synthesis, assignment of the relative and absolute stereochemistry, and structural reassignment of phostriecin (aka Sultriecin).
Journal of the American Chemical Society 2010;132(7):2157-9.
2010: Mauro Mileni; Joie Garfunkle; Cyrine Ezzili; F Scott Kimball; Benjamin F Cravatt; Raymond C Stevens; Dale L Boger
X-ray crystallographic analysis of alpha-ketoheterocycle inhibitors bound to a humanized variant of fatty acid amide hydrolase.
Journal of medicinal chemistry 2010;53(1):230-40.
2010: Vidya Subramanian; Robert M Williams; Dale L Boger; Karolin Luger
Methods to characterize the effect of DNA-modifying compounds on nucleosomal DNA.
Methods in molecular biology (Clifton, N.J.) 2010;613():173-92.
2009: Karen S MacMillan; James P Lajiness; Carlota Lopez Cara; Romeo Romagnoli; William M Robertson; Inkyu Hwang; Pier Giovanni Baraldi; Dale L Boger
Synthesis and evaluation of a thio analogue of duocarmycin SA.
Bioorganic & medicinal chemistry letters 2009;19(24):6962-5.
2009: Joie Garfunkle; F Scott Kimball; John D Trzupek; Shinobu Takizawa; Hiroyuki Shimamura; Masaki Tomishima; Dale L Boger
Total synthesis of chloropeptin II (complestatin) and chloropeptin I.
Journal of the American Chemical Society 2009;131(44):16036-8.
2009: Jin Shi; James S Stover; Landon R Whitby; Peter K Vogt; Dale L Boger
Small molecule inhibitors of Myc/Max dimerization and Myc-induced cell transformation.
Bioorganic & medicinal chemistry letters 2009;19(21):6038-41.
2009: Xiao Fang; Joonwoo Nam; Dongwoo Shin; Yosup Rew; Dale L Boger; Suzanne Walker
Functional and biochemical analysis of a key series of ramoplanin analogues.
Bioorganic & medicinal chemistry letters 2009;19(21):6189-91.
2009: Karen S MacMillan; Dale L Boger
Fundamental relationships between structure, reactivity, and biological activity for the duocarmycins and CC-1065.
Journal of medicinal chemistry 2009;52(19):5771-80.
2009: Mark R Swingle; Lauren Amable; Brian G Lawhorn; Suzanne B Buck; Christopher P Burke; Pukar Ratti; Kimberly L Fischer; Dale L Boger; Richard E Honkanen
Structure-activity relationship studies of fostriecin, cytostatin, and key analogs, with PP1, PP2A, PP5, and( beta12-beta13)-chimeras (PP1/PP2A and PP5/PP2A), provide further insight into the inhibitory actions of fostriecin family inhibitors.
The Journal of pharmacology and experimental therapeutics 2009;331(1):45-53.
2009: S G Kinsey; J Z Long; S T O'Neal; R A Abdullah; Justin L Poklis; Dale L Boger; Benjamin F Cravatt; Aron H Lichtman
Blockade of endocannabinoid-degrading enzymes attenuates neuropathic pain.
The Journal of pharmacology and experimental therapeutics 2009;330(3):902-10.
2009: Mauro Mileni; Joie Garfunkle; Jessica K DeMartino; Benjamin F Cravatt; Dale L Boger; Raymond C Stevens
Binding and inactivation mechanism of a humanized fatty acid amide hydrolase by alpha-ketoheterocycle inhibitors revealed from cocrystal structures.
Journal of the American Chemical Society 2009;131(30):10497-506.
2009: Landon R Whitby; Andrew M Lee; Stefan Kunz; Michael B A Oldstone; Dale L Boger
Characterization of lassa virus cell entry inhibitors: determination of the active enantiomer by asymmetric synthesis.
Bioorganic & medicinal chemistry letters 2009;19(14):3771-4.
2009: Alex Shaginian; Landon R Whitby; Sukwon Hong; Inkyu Hwang; Bilal Farooqi; Mark Searcey; Jiandong Chen; Peter K Vogt; Dale L Boger
Design, synthesis, and evaluation of an alpha-helix mimetic library targeting protein-protein interactions.
Journal of the American Chemical Society 2009;131(15):5564-72.
2009: Hayato Ishikawa; David A Colby; Shigeki Seto; Porino Va; Annie Tam; Hiroyuki Kakei; Thomas J Rayl; Inkyu Hwang; Dale L Boger
Total synthesis of vinblastine, vincristine, related natural products, and key structural analogues.
Journal of the American Chemical Society 2009;131(13):4904-16.
2009: Ryan C Clark; Sang Yeul Lee; Mark Searcey; Dale L Boger
The isolation, total synthesis and structure elucidation of chlorofusin, a natural product inhibitor of the p53-mDM2 protein-protein interaction.
Natural product reports 2009;26(4):465-77.
2009: Joel E Schlosburg; Dale L Boger; Benjamin F Cravatt; Aron H Lichtman
Endocannabinoid modulation of scratching response in an acute allergenic model: a new prospective neural therapeutic target for pruritus.
The Journal of pharmacology and experimental therapeutics 2009;329(1):314-23.
2009: Christine M Crane; Dale L Boger
Synthesis and evaluation of vancomycin aglycon analogues that bear modifications in the N-terminal D-leucyl amino acid.
Journal of medicinal chemistry 2009;52(5):1471-6.
2009: James S Stover; Jin Shi; Wei Jin; Peter K Vogt; Dale L Boger
Discovery of inhibitors of aberrant gene transcription from Libraries of DNA binding molecules: inhibition of LEF-1-mediated gene transcription and oncogenic transformation.
Journal of the American Chemical Society 2009;131(9):3342-8.
2009: Karen S MacMillan; Trihn Nguyen; Inkyu Hwang; Dale L Boger
Total synthesis and evaluation of iso-duocarmycin SA and iso-yatakemycin.
Journal of the American Chemical Society 2009;131(3):1187-94.
2008: Karen S MacMillan; Dale L Boger
An additional spirocyclization for duocarmycin SA.
Journal of the American Chemical Society 2008;130(49):16521-3.
2008: Ian M Slaymaker; Michael Bracey; Mauro Mileni; Joie Garfunkle; Benjamin F Cravatt; Dale L Boger; Raymond C Stevens
Correlation of inhibitor effects on enzyme activity and thermal stability for the integral membrane protein fatty acid amide hydrolase.
Bioorganic & medicinal chemistry letters 2008;18(22):5847-50.
2008: Jessica K DeMartino; Joie Garfunkle; Dustin G Hochstatter; Benjamin F Cravatt; Dale L Boger
Exploration of a fundamental substituent effect of alpha-ketoheterocycle enzyme inhibitors: Potent and selective inhibitors of fatty acid amide hydrolase.
Bioorganic & medicinal chemistry letters 2008;18(22):5842-6.
2008: Ryan C Clark; Sang Yeul Lee; Dale L Boger
Total synthesis of chlorofusin, its seven chromophore diastereomers, and key partial structures.
Journal of the American Chemical Society 2008;130(37):12355-69.
2008: Jessica K DeMartino; Inkyu Hwang; Stephen Connelly; Ian A Wilson; Dale L Boger
Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase.
Journal of medicinal chemistry 2008;51(17):5441-8.
2008: Joie Garfunkle; Cyrine Ezzili; Thomas J Rayl; Dustin G Hochstatter; Inkyu Hwang; Dale L Boger
Optimization of the central heterocycle of alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase.
Journal of medicinal chemistry 2008;51(15):4392-403.
2008: Andrew M Lee; Jillian M Rojek; Christina F Spiropoulou; Anette T Gundersen; Wei Jin; Alex Shaginian; Joanne York; Jack H Nunberg; Dale L Boger; Michael B A Oldstone; Stefan Kunz
Unique small molecule entry inhibitors of hemorrhagic fever arenaviruses.
The Journal of biological chemistry 2008;283(27):18734-42.
2008: Mark S Tichenor; Dale L Boger
Yatakemycin: total synthesis, DNA alkylation, and biological properties.
Natural product reports 2008;25(2):220-6.
2008: Xiaohong Lu; Peter K Vogt; Dale L Boger; John Lunec
Disruption of the MYC transcriptional function by a small-molecule antagonist of MYC/MAX dimerization.
Oncology reports 2008;19(3):825-30.
2008: F Scott Kimball; F Anthony Romero; Cyrine Ezzili; Joie Garfunkle; Thomas J Rayl; Dustin G Hochstatter; Inkyu Hwang; Dale L Boger
Optimization of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.
Journal of medicinal chemistry 2008;51(4):937-47.
2008: Hayato Ishikawa; David A Colby; Dale L Boger
Direct coupling of catharanthine and vindoline to provide vinblastine: total synthesis of (+)- and ent-(-)-vinblastine.
Journal of the American Chemical Society 2008;130(2):420-1.
2007: Wei Jin; John D Trzupek; Thomas J Rayl; Melinda A Broward; George A Vielhauer; Scott J Weir; Inhwan Hwang; Dale L Boger
A unique class of duocarmycin and CC-1065 analogues subject to reductive activation.
Journal of the American Chemical Society 2007;129(49):15391-7.
2007: Mark S Tichenor; Karen S MacMillan; James S Stover; Scott E Wolkenberg; Maria G Pavani; Lorenzo Zanella; Abdel N Zaid; Gianpiero Spalluto; Thomas J Rayl; Inhwan Hwang; Pier Giovanni Baraldi; Dale L Boger
Rational design, synthesis, and evaluation of key analogues of CC-1065 and the duocarmycins.
Journal of the American Chemical Society 2007;129(45):14092-9.
2007: Mark S Tichenor; Karen S MacMillan; John D Trzupek; Thomas J Rayl; Inhwan Hwang; Dale L Boger
Systematic exploration of the structural features of yatakemycin impacting DNA alkylation and biological activity.
Journal of the American Chemical Society 2007;129(35):10858-69.
2007: Sang Yeul Lee; Ryan C Clark; Dale L Boger
Total synthesis, stereochemical reassignment, and absolute configuration of chlorofusin.
Journal of the American Chemical Society 2007;129(32):9860-1.
2007: Joonwoo Nam; Dongwoo Shin; Yosup Rew; Dale L Boger
Alanine scan of [L-Dap(2)]ramoplanin A2 aglycon: assessment of the importance of each residue.
Journal of the American Chemical Society 2007;129(28):8747-55.
2007: Christophe Hardouin; Michael J Kelso; F Anthony Romero; Thomas J Rayl; Donmienne Leung; Inhwan Hwang; Benjamin F Cravatt; Dale L Boger
Structure-activity relationships of alpha-ketooxazole inhibitors of fatty acid amide hydrolase.
Journal of medicinal chemistry 2007;50(14):3359-68.
2007: Lan Xu; Youhoon Chong; Inhwan Hwang; Anthony D'Onofrio; Kristen Amore; G Peter Beardsley; Chenglong Li; Arthur J Olson; Dale L Boger; Ian A Wilson
Structure-based design, synthesis, evaluation, and crystal structures of transition state analogue inhibitors of inosine monophosphate cyclohydrolase.
The Journal of biological chemistry 2007;282(17):13033-46.
2007: F Anthony Romero; Wu Du; Inhwan Hwang; Thomas J Rayl; F Scott Kimball; Donmienne Leung; Heather S Hoover; Richard L Apodaca; J Guy Breitenbucher; Benjamin F Cravatt; Dale L Boger
Potent and selective alpha-ketoheterocycle-based inhibitors of the anandamide and oleamide catabolizing enzyme, fatty acid amide hydrolase.
Journal of medicinal chemistry 2007;50(5):1058-68.
2007: Lisa M Eubanks; Mark Hixon; Wei Jin; Sukwon Hong; Colin M Clancy; William H Tepp; Michael R Baldwin; Carl J Malizio; Michael C Goodnough; Joseph T Barbieri; Eric A Johnson; Dale L Boger; Tobin J Dickerson; Kim D Janda
An in vitro and in vivo disconnect uncovered through high-throughput identification of botulinum neurotoxin A antagonists.
Proceedings of the National Academy of Sciences of the United States of America 2007;104(8):2602-7.
2006: Brian G Lawhorn; Sobhana B Boga; Scott E Wolkenberg; David A Colby; Carla-Marie Gauss; Mark R Swingle; Lauren Amable; Richard E Honkanen; Dale L Boger
Total synthesis and evaluation of cytostatin, its C10-C11 diastereomers, and additional key analogues: impact on PP2A inhibition.
Journal of the American Chemical Society 2006;128(51):16720-32.
2006: Mark S Tichenor; John D Trzupek; David B Kastrinsky; Futoshi Shiga; Inhwan Hwang; Dale L Boger
Asymmetric total synthesis of (+)- and ent-(-)-yatakemycin and duocarmycin SA: evaluation of yatakemycin key partial structures and its unnatural enantiomer.
Journal of the American Chemical Society 2006;128(49):15683-96.
2006: F Anthony Romero; Inhwan Hwang; Dale L Boger
Delineation of a fundamental alpha-ketoheterocycle substituent effect for use in the design of enzyme inhibitors.
Journal of the American Chemical Society 2006;128(43):14004-5.
2006: Martin J Schnermann; F Anthony Romero; Inhwan Hwang; Eiko Nakamaru-Ogiso; Takao Yagi; Dale L Boger
Total synthesis of piericidin A1 and B1 and key analogues.
Journal of the American Chemical Society 2006;128(36):11799-807.
2006: Hayato Ishikawa; Gregory I Elliott; Juraj Velcicky; Younggi Choi; Dale L Boger
Total synthesis of (-)- and ent-(+)-vindoline and related alkaloids.
Journal of the American Chemical Society 2006;128(32):10596-612.
2006: Gregory I Elliott; James R Fuchs; Brian S J Blagg; Hayato Ishikawa; Houchao Tao; Z-Q Yuan; Dale L Boger
Intramolecular diels-alder/1,3-dipolar cycloaddition cascade of 1,3,4-oxadiazoles.
Journal of the American Chemical Society 2006;128(32):10589-95.
2006: Jessica K DeMartino; Inhwan Hwang; Lan Xu; Ian A Wilson; Dale L Boger
Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase.
Journal of medicinal chemistry 2006;49(10):2998-3002.
2006: Brendan M Crowley; Dale L Boger
Total synthesis and evaluation of [Psi[CH2NH]Tpg4]vancomycin aglycon: reengineering vancomycin for dual D-Ala-D-Ala and D-Ala-D-Lac binding.
Journal of the American Chemical Society 2006;128(9):2885-92.
2006: Ryan C Clark; Steven S Pfeiffer; Dale L Boger
Diastereoselective Diels-Alder reactions of N-sulfonyl-1-aza-1,3-butadienes with optically active enol ethers: an asymmetric variant of the 1-azadiene Diels-Alder reaction.
Journal of the American Chemical Society 2006;128(8):2587-93.
2006: John D Trzupek; Joel M Gottesfeld; Dale L Boger
Alkylation of duplex DNA in nucleosome core particles by duocarmycin SA and yatakemycin.
Nature chemical biology 2006;2(2):79-82.
2006: Gregory I Elliott; Juraj Velcicky; Hayato Ishikawa; Yongkai Li; Dale L Boger
Total synthesis of (-)- and ent-(+)-vindorosine: tandem intramolecular Diels-Alder/1,3-dipolar cycloaddition of 1,3,4-oxadiazoles.
Angewandte Chemie (International ed. in English) 2006;45(4):620-2.
2006: Akiyuki Hamasaki; Richard Ducray; Dale L Boger
Two novel 1,2,4,5-tetrazines that participate in inverse electron demand Diels-Alder reactions with an unexpected regioselectivity.
The Journal of organic chemistry 2006;71(1):185-93.
2005: Cristiano Ruch Werneck Guimarães; Dale L Boger; William L Jorgensen
Elucidation of fatty acid amide hydrolase inhibition by potent alpha-ketoheterocycle derivatives from Monte Carlo simulations.
Journal of the American Chemical Society 2005;127(49):17377-84.
2005: Martin J Schnermann; Dale L Boger
Total synthesis of piericidin A1 and B1.
Journal of the American Chemical Society 2005;127(45):15704-5.
2005: Ting-Chao Chou; Yongbiao Guan; Danielle R Soenen; Samuel J Danishefsky; Dale L Boger
Potent reversal of multidrug resistance by ningalins and its use in drug combinations against human colon carcinoma xenograft in nude mice.
Cancer chemotherapy and pharmacology 2005;56(4):379-90.
2005: Younggi Choi; Hayato Ishikawa; Juraj Velcicky; Gregory I Elliott; Michael M Miller; Dale L Boger
Total synthesis of (-)- and ent-(+)-vindoline.
Organic letters 2005;7(20):4539-42.
2005: Akiyuki Hamasaki; Jeffrey M Zimpleman; Inhwan Hwang; Dale L Boger
Total synthesis of ningalin D.
Journal of the American Chemical Society 2005;127(30):10767-70.
2005: Kevin Capps; Jon Humiston; Romyr Dominique; Inhwan Hwang; Dale L Boger
Discovery of AICAR Tfase inhibitors that disrupt requisite enzyme dimerization.
Bioorganic & medicinal chemistry letters 2005;15(11):2840-4.
2005: Heng Cheng; Inhwan Hwang; Youhoon Chong; Ali Tavassoli; Michael E Webb; Yan Zhang; Ian A Wilson; Stephen J Benkovic; Dale L Boger
Synthesis and biological evaluation of N-[4-[5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoroacetyl)pentyl]benzoyl]-L-glutamic acid as a potential inhibitor of GAR Tfase and the de novo purine biosynthetic pathway.
Bioorganic & medicinal chemistry 2005;13(10):3593-9.
2005: Youhoon Chong; Inhwan Hwang; Ali Tavassoli; Yan Zhang; Ian A Wilson; Stephen J Benkovic; Dale L Boger
Synthesis and biological evaluation of alpha- and gamma-carboxamide derivatives of 10-CF3CO-DDACTHF.
Bioorganic & medicinal chemistry 2005;13(10):3587-92.
2005: Heng Cheng; Youhoon Chong; Inhwan Hwang; Ali Tavassoli; Yan Zhang; Ian A Wilson; Stephen J Benkovic; Dale L Boger
Design, synthesis, and biological evaluation of 10-methanesulfonyl-DDACTHF, 10-methanesulfonyl-5-DACTHF, and 10-methylthio-DDACTHF as potent inhibitors of GAR Tfase and the de novo purine biosynthetic pathway.
Bioorganic & medicinal chemistry 2005;13(10):3577-85.
2005: Winston C Tse; Dale L Boger
A fluorescent intercalator displacement assay for establishing DNA binding selectivity and affinity.
Current protocols in nucleic acid chemistry / edited by Serge L. Beaucage ... [et al.] 2005;Chapter 8():Unit 8.5.
2005: Dale L Boger; Hiroshi Miyauchi; Wu Du; Christophe Hardouin; Robert A Fecik; Heng Cheng; Inhwan Hwang; Michael P Hedrick; Donmienne Leung; Orlando Acevedo; Cristiano Ruch Werneck Guimarães; William L Jorgensen; Benjamin F Cravatt
Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.
Journal of medicinal chemistry 2005;48(6):1849-56.
2005: Donmienne Leung; Wu Du; Christophe Hardouin; Heng Cheng; Inhwan Hwang; Benjamin F Cravatt; Dale L Boger
Discovery of an exceptionally potent and selective class of fatty acid amide hydrolase inhibitors enlisting proteome-wide selectivity screening: concurrent optimization of enzyme inhibitor potency and selectivity.
Bioorganic & medicinal chemistry letters 2005;15(5):1423-8.
2005: Zhong Qing Yuan; Hayato Ishikawa; Dale L Boger
Total synthesis of natural (+)- [corrected] and ent-(-)-4-desacetoxy-6,7-dihydrovindorosine [corrected] and natural and ent-minovine: oxadiazole tandem intramolecular Diels-Alder/1,3-dipolar cycloaddition reaction.
Organic letters 2005;7(4):741-4.
2005: Suzanne Walker; Lan Chen; Yanan Hu; Yosup Rew; Dongwoo Shin; Dale L Boger
Chemistry and biology of ramoplanin: a lipoglycodepsipeptide with potent antibiotic activity.
Chemical reviews 2005;105(2):449-76.
2005: Wu Du; Christophe Hardouin; Heng Cheng; Inhwan Hwang; Dale L Boger
Heterocyclic sulfoxide and sulfone inhibitors of fatty acid amide hydrolase.
Bioorganic & medicinal chemistry letters 2005;15(1):103-6.
2004: Houchao Tao; Inhwan Hwang; Dale L Boger
Multidrug resistance reversal activity of permethyl ningalin B amide derivatives.
Bioorganic & medicinal chemistry letters 2004;14(24):5979-81.
2004: Winston C Tse; Dale L Boger
Sequence-selective DNA recognition: natural products and nature's lessons.
Chemistry & biology 2004;11(12):1607-17.
2004: Jay P Parrish; John D Trzupek; Terry V Hughes; Inhwan Hwang; Dale L Boger
Synthesis and evaluation of N-aryl and N-alkenyl CBI derivatives.
Bioorganic & medicinal chemistry 2004;12(22):5845-56.
2004: Aron H Lichtman; Donmienne Leung; Christopher C Shelton; Alan Saghatelian; Christophe Hardouin; Dale L Boger; Benjamin F Cravatt
Reversible inhibitors of fatty acid amide hydrolase that promote analgesia: evidence for an unprecedented combination of potency and selectivity.
The Journal of pharmacology and experimental therapeutics 2004;311(2):441-8.
2004: Dongwoo Shin; Yosup Rew; Dale L Boger
Total synthesis and structure of the ramoplanin A1 and A3 aglycons: two minor components of the ramoplanin complex.
Proceedings of the National Academy of Sciences of the United States of America 2004;101(33):11977-9.
2004: Patrick S Lee; Wu Du; Dale L Boger; William L Jorgensen
Energetic preferences for alpha,beta versus beta,gamma unsaturation.
The Journal of organic chemistry 2004;69(16):5448-53.
2004: Young-Wan Ham; Dale L Boger
A powerful selection assay for mixture libraries of DNA alkylating agents.
Journal of the American Chemical Society 2004;126(30):9194-5.
2004: Mark S Tichenor; David B Kastrinsky; Dale L Boger
Total synthesis, structure revision, and absolute configuration of (+)-yatakemycin.
Journal of the American Chemical Society 2004;126(27):8396-8.
2004: Antonietta Lillo; Chengzao Sun; Changshou Gao; Henrik J Ditzel; Jay Parrish; Carla-Marie Gauss; Jason Moss; Brunhilde Felding-Habermann; Peter Wirsching; Dale L Boger; Kim D Janda
A human single-chain antibody specific for integrin alpha3beta1 capable of cell internalization and delivery of antitumor agents.
Chemistry & biology 2004;11(7):897-906.
2004: Lan Chen; Yanqiu Yuan; Jeremiah S Helm; Yanan Hu; Yosup Rew; Dongwoo Shin; Dale L Boger; Suzanne Walker
Dissecting ramoplanin: mechanistic analysis of synthetic ramoplanin analogues as a guide to the design of improved antibiotics.
Journal of the American Chemical Society 2004;126(24):7462-3.
2004: Brendan M Crowley; Yoshiki Mori; Casey C McComas; Datong Tang; Dale L Boger
Total synthesis of the ristocetin aglycon.
Journal of the American Chemical Society 2004;126(13):4310-7.
2004: David B Kastrinsky; Dale L Boger
Effective asymmetric synthesis of 1,2,9,9a-tetrahydrocyclopropa[c]benzo[e]indol-4-one (CBI).
The Journal of organic chemistry 2004;69(7):2284-9.
2004: Yosup Rew; Dongwoo Shin; Inhwan Hwang; Dale L Boger
Total synthesis and examination of three key analogues of ramoplanin: a lipoglycodepsipeptide with potent antibiotic activity.
Journal of the American Chemical Society 2004;126(4):1041-3.
2004: Jay P Parrish; Terry V Hughes; Inhwan Hwang; Dale L Boger
Establishing the parabolic relationship between reactivity and activity for derivatives and analogues of the duocarmycin and CC-1065 alkylation subunits.
Journal of the American Chemical Society 2004;126(1):80-1.
2004: Winston C Tse; Dale L Boger
A fluorescent intercalator displacement assay for establishing DNA binding selectivity and affinity.
Accounts of chemical research 2004;37(1):61-9.
2003: Pankaj Desai; Steven S Pfeiffer; Dale L Boger
Synthesis of the chlorofusin cyclic peptide: assignment of the asparagine stereochemistry.
Organic letters 2003;5(26):5047-50.
2003: Suzanne B Buck; Christophe Hardouin; Satoshi Ichikawa; Danielle R Soenen; Carla-Marie Gauss; Inhwan Hwang; Mark R Swingle; Kathy M Bonness; Richard E Honkanen; Dale L Boger
Fundamental role of the fostriecin unsaturated lactone and implications for selective protein phosphatase inhibition.
Journal of the American Chemical Society 2003;125(51):15694-5.
2003: Jay P Parrish; David B Kastrinsky; Inhwan Hwang; Dale L Boger
Synthesis and evaluation of duocarmycin and CC-1065 analogues incorporating the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]-3-azaindol-4-one (CBA) alkylation subunit.
The Journal of organic chemistry 2003;68(23):8984-90.
2003: Carla Bassarello; Paola Cimino; Giuseppe Bifulco; Dale L Boger; Jarrod A Smith; Walter J Chazin; Luigi Gomez-Paloma
NMR structure of the (+)-CPI-indole/d(GACTAATTGAC)-d(GTCAATTAGTC) covalent complex.
Chembiochem : a European journal of chemical biology 2003;4(11):1188-93.
2003: Young-Wan Ham; Winston C Tse; Dale L Boger
High-resolution assessment of protein DNA binding affinity and selectivity utilizing a fluorescent intercalator displacement (FID) assay.
Bioorganic & medicinal chemistry letters 2003;13(21):3805-7.
2003: Bryan K S Yeung; Winston C Tse; Dale L Boger
Determination of binding affinities of triplex forming oligonucleotides using a fluorescent intercalator displacement (FID) assay.
Bioorganic & medicinal chemistry letters 2003;13(21):3801-4.
2003: Joel Desharnais; Inhwan Hwang; Yan Zhang; Ali Tavassoli; Justin Baboval; Stephen J Benkovic; Ian A Wilson; Dale L Boger
Design, synthesis and biological evaluation of 10-CF3CO-DDACTHF analogues and derivatives as inhibitors of GAR Tfase and the de novo purine biosynthetic pathway.
Bioorganic & medicinal chemistry 2003;11(20):4511-21.
2003: Thomas H Marsilje; Michael P Hedrick; Joel Desharnais; Kevin Capps; Ali Tavassoli; Yan Zhang; Ian A Wilson; Stephen J Benkovic; Dale L Boger
10-(2-benzoxazolcarbonyl)-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid: a potential inhibitor of GAR transformylase and AICAR transformylase.
Bioorganic & medicinal chemistry 2003;11(20):4503-9.
2003: Thomas H Marsilje; Michael P Hedrick; Joel Desharnais; Ali Tavassoli; Yan Zhang; Ian A Wilson; Stephen J Benkovic; Dale L Boger
Design, synthesis, and biological evaluation of simplified alpha-keto heterocycle, trifluoromethyl ketone, and formyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.
Bioorganic & medicinal chemistry 2003;11(20):4487-501.
2003: Winston C Tse; Takahiro Ishii; Dale L Boger
Comprehensive high-resolution analysis of hairpin polyamides utilizing a fluorescent intercalator displacement (FID) assay.
Bioorganic & medicinal chemistry 2003;11(20):4479-86.
2003: Dale L Boger; Joel Desharnais; Kevin Capps
Solution-phase combinatorial libraries: modulating cellular signaling by targeting protein-protein or protein-DNA interactions.
Angewandte Chemie (International ed. in English) 2003;42(35):4138-76.
2003: Jay P Parrish; David B Kastrinsky; Scott E Wolkenberg; Yasuhiro Igarashi; Dale L Boger
DNA alkylation properties of yatakemycin.
Journal of the American Chemical Society 2003;125(36):10971-6.
2003: Casey C McComas; Brendan M Crowley; Inhwan Hwang; Dale L Boger
Synthesis and evaluation of methyl ether derivatives of the vancomycin, teicoplanin, and ristocetin aglycon methyl esters.
Bioorganic & medicinal chemistry letters 2003;13(17):2933-6.
2003: Jay P Parrish; David B Kastrinsky; Frederic Stauffer; Michael P Hedrick; Inhwan Hwang; Dale L Boger
Establishment of substituent effects in the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065.
Bioorganic & medicinal chemistry 2003;11(17):3815-38.
2003: Casey C McComas; Brendan M Crowley; Dale L Boger
Partitioning the loss in vancomycin binding affinity for D-Ala-D-Lac into lost H-bond and repulsive lone pair contributions.
Journal of the American Chemical Society 2003;125(31):9314-5.
2003: Jay P Parrish; David B Kastrinsky; Dale L Boger
Synthesis and X-ray analysis of an unprecedented and stable 2-aza-4,4-spirocyclopropacyclohexadienone.
Organic letters 2003;5(14):2577-9.
2003: Bryan K S Yeung; Dale L Boger
Synthesis of isochrysohermidin-distamycin hybrids.
The Journal of organic chemistry 2003;68(13):5249-53.
2003: Donmienne Leung; Christophe Hardouin; Dale L Boger; Benjamin F Cravatt
Discovering potent and selective reversible inhibitors of enzymes in complex proteomes.
Nature biotechnology 2003;21(6):687-91.
2003: Yan Zhang; Joel Desharnais; Thomas H Marsilje; Chenglong Li; Michael P Hedrick; Lata T Gooljarsingh; Ali Tavassoli; Stephen J Benkovic; Arthur J Olson; Dale L Boger; Ian A Wilson
Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid.
Biochemistry 2003;42(20):6043-56.
2003: Danielle R Soenen; Inhwan Hwang; Michael P Hedrick; Dale L Boger
Multidrug resistance reversal activity of key ningalin analogues.
Bioorganic & medicinal chemistry letters 2003;13(10):1777-81.
2003: Danielle R Soenen; Jeffrey M Zimpleman; Dale L Boger
Synthesis and inverse electron demand Diels-Alder reactions of 3,6-bis(3,4-dimethoxybenzoyl)-1,2,4,5-tetrazine.
The Journal of organic chemistry 2003;68(9):3593-8.
2003: Dale L Boger
Solution-phase synthesis of combinatorial libraries designed to modulate protein-protein or protein-DNA interactions.
Bioorganic & medicinal chemistry 2003;11(8):1607-13.
2003: Jutta Wanner; Datong Tang; Casey C McComas; Brendan M Crowley; Wanlong Jiang; Jason Moss; Dale L Boger
A new and improved method for deglycosidation of glycopeptide antibiotics exemplified with vancomycin, ristocetin, and ramoplanin.
Bioorganic & medicinal chemistry letters 2003;13(6):1169-73.
2003: Wanlong Jiang; Jutta Wanner; Richard J Lee; Pierre-Yves Bounaud; Dale L Boger
Total synthesis of the ramoplanin A2 and ramoplanose aglycon.
Journal of the American Chemical Society 2003;125(7):1877-87.
2002: Yan Zhang; Joel Desharnais; Samantha E Greasley; G Peter Beardsley; Dale L Boger; Ian A Wilson
Crystal structures of human GAR Tfase at low and high pH and with substrate beta-GAR.
Biochemistry 2002;41(48):14206-15.
2002: Yves Ambroise; Brian Yaspan; Mark H Ginsberg; Dale L Boger
Inhibitors of cell migration that inhibit intracellular paxillin/alpha4 binding: a well-documented use of positional scanning libraries.
Chemistry & biology 2002;9(11):1219-26.
2002: D S Lewy; Carla-Marie Gauss; Danielle R Soenen; Dale L Boger
Fostriecin: chemistry and biology.
Current medicinal chemistry 2002;9(22):2005-32.
2002: Scott E Wolkenberg; Dale L Boger
Total synthesis of anhydrolycorinone utilizing sequential intramolecular Diels-Alder reactions of a 1,3,4-oxadiazole.
The Journal of organic chemistry 2002;67(21):7361-4.
2002: Gordon D Wilkie; Gregory I Elliott; Brian S J Blagg; Scott E Wolkenberg; Danielle R Soenen; Michael M Miller; Scott Pollack; Dale L Boger
Intramolecular Diels-Alder and tandem intramolecular Diels-Alder/1,3-dipolar cycloaddition reactions of 1,3,4-oxadiazoles.
Journal of the American Chemical Society 2002;124(38):11292-4.
2002: Craig R Woods; Nicolas Faucher; Bernd Eschgfaller; Kenneth W Bair; Dale L Boger
Synthesis and DNA binding properties of saturated distamycin analogues.
Bioorganic & medicinal chemistry letters 2002;12(18):2647-50.
2002: Craig R Woods; Takahiro Ishii; Dale L Boger
Synthesis and DNA binding properties of iminodiacetic acid-linked polyamides: characterization of cooperative extended 2:1 side-by-side parallel binding.
Journal of the American Chemical Society 2002;124(36):10676-82.
2002: Thomas H Marsilje; Marc A Labroli; Michael P Hedrick; Qing Jin; Joel Desharnais; Stephen J Baker; Lata T Gooljarsingh; Joseph Ramcharan; Ali Tavassoli; Yan Zhang; Ian A Wilson; G Peter Beardsley; Stephen J Benkovic; Dale L Boger
10-Formyl-5,10-dideaza-acyclic-5,6,7,8-tetrahydrofolic acid (10-formyl-DDACTHF): a potent cytotoxic agent acting by selective inhibition of human GAR Tfase and the de novo purine biosynthetic pathway.
Bioorganic & medicinal chemistry 2002;10(8):2739-49.
2002: Scott E Wolkenberg; Dale L Boger
Mechanisms of in situ activation for DNA-targeting antitumor agents.
Chemical reviews 2002;102(7):2477-95.
2002: Yan Chen; Martin Bilban; Carolyn A Foster; Dale L Boger
Solution-phase parallel synthesis of a pharmacophore library of HUN-7293 analogues: a general chemical mutagenesis approach to defining structure-function properties of naturally occurring cyclic (depsi)peptides.
Journal of the American Chemical Society 2002;124(19):5431-40.
2002: Wanlong Jiang; Jutta Wanner; Richard J Lee; Pierre-Yves Bounaud; Dale L Boger
Total synthesis of the ramoplanin A2 and ramoplanose aglycon.
Journal of the American Chemical Society 2002;124(19):5288-90.
2002: J Jeffrey McAtee; Steven L Castle; Qing Jin; Dale L Boger
Synthesis and evaluation of vancomycin and vancomycin aglycon analogues that bear modifications in the residue 3 asparagine.
Bioorganic & medicinal chemistry letters 2002;12(9):1319-22.
2002: Thorsten Berg; Steven B Cohen; Joel Desharnais; Corinna K Sonderegger; Daniel J Maslyar; Joel Goldberg; Dale L Boger; Peter K Vogt
Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts.
Proceedings of the National Academy of Sciences of the United States of America 2002;99(6):3830-5.
2002: Craig R Woods; Takahiro Ishii; Bing Wu; Kenneth W Bair; Dale L Boger
Hairpin versus extended DNA binding of a substituted beta-alanine linked polyamide.
Journal of the American Chemical Society 2002;124(10):2148-52.
2002: Yves Ambroise; Dale L Boger
The DNA phosphate backbone is not involved in catalysis of the duocarmycin and CC-1065 DNA alkylation reaction.
Bioorganic & medicinal chemistry letters 2002;12(3):303-6.
2002: Joel Goldberg; Qing Jin; Yves Ambroise; Shigeki Satoh; Joel Desharnais; Kevin Capps; Dale L Boger
Erythropoietin mimetics derived from solution phase combinatorial libraries.
Journal of the American Chemical Society 2002;124(4):544-55.
2001: Samantha E Greasley; Thomas H Marsilje; H Cai; S Baker; Stephen J Benkovic; Dale L Boger; Ian A Wilson
Unexpected formation of an epoxide-derived multisubstrate adduct inhibitor on the active site of GAR transformylase.
Biochemistry 2001;40(45):13538-47.
2001: Dale L Boger; H W Schmitt; BE Fink; Michael P Hedrick
Parallel synthesis and evaluation of 132 (+)-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) analogues of CC-1065 and the duocarmycins defining the contribution of the DNA-binding domain.
The Journal of organic chemistry 2001;66(20):6654-61.
2001: Irina Fedorova; A Hashimoto; Robert A Fecik; Michael P Hedrick; LO Hanus; Dale L Boger; Kenner C Rice; Anthony Basile
Behavioral evidence for the interaction of oleamide with multiple neurotransmitter systems.
The Journal of pharmacology and experimental therapeutics 2001;299(1):332-42.
2001: D A Ellis; Scott E Wolkenberg; Dale L Boger
Metal cation complexation and activation of reversed CPyI analogues of CC-1065 and duocarmycin SA: partitioning the effects of binding and catalysis.
Journal of the American Chemical Society 2001;123(38):9299-306.
2001: Dale L Boger; J Hong
Asymmetric total synthesis of ent-(-)-roseophilin: assignment of absolute configuration.
Journal of the American Chemical Society 2001;123(35):8515-9.
2001: Dale L Boger
Vancomycin, teicoplanin, and ramoplanin: synthetic and mechanistic studies.
Medicinal research reviews 2001;21(5):356-81.
2001: Dale L Boger; Winston C Tse
Thiazole orange as the fluorescent intercalator in a high resolution fid assay for determining DNA binding affinity and sequence selectivity of small molecules.
Bioorganic & medicinal chemistry 2001;9(9):2511-8.
2001: Dale L Boger; F Stauffer; Michael P Hedrick
Substituent effects within the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065.
Bioorganic & medicinal chemistry letters 2001;11(15):2021-4.
2001: Dale L Boger; SR Brunette; R M Garbaccio
Synthesis and evaluation of a series of C3-substituted CBI analogues of CC-1065 and the duocarmycins.
The Journal of organic chemistry 2001;66(15):5163-73.
2001: Dale L Boger; BE Fink; SR Brunette; Winston C Tse; Michael P Hedrick
A simple, high-resolution method for establishing DNA binding affinity and sequence selectivity.
Journal of the American Chemical Society 2001;123(25):5878-91.
2001: Dale L Boger; Hiroshi Miyauchi; Michael P Hedrick
alpha-Keto heterocycle inhibitors of fatty acid amide hydrolase: carbonyl group modification and alpha-substitution.
Bioorganic & medicinal chemistry letters 2001;11(12):1517-20.
2001: Dale L Boger; Satoshi Ichikawa; W Zhong
Total synthesis of fostriecin (CI-920).
Journal of the American Chemical Society 2001;123(18):4161-7.
2001: Dale L Boger; Terry V Hughes; Michael P Hedrick
Synthesis, chemical properties, and biological evaluation of CC-1065 and duocarmycin analogues incorporating the 5-methoxycarbonyl-1,2,9,9a-tetrahydrocyclopropa.
The Journal of organic chemistry 2001;66(7):2207-16.
2001: Dale L Boger; S H Kim; Y Mori; J H Weng; O Rogel; Steven L Castle; J J McAtee
First and second generation total synthesis of the teicoplanin aglycon.
Journal of the American Chemical Society 2001;123(9):1862-71.
2001: Dale L Boger; Joel Goldberg
Cytokine receptor dimerization and activation: prospects for small molecule agonists.
Bioorganic & medicinal chemistry 2001;9(3):557-62.
2001: Dale L Boger; Joel Goldberg; Steven A. Silletti; Torsten Kessler; David A Cheresh
Identification of a novel class of small-molecule antiangiogenic agents through the screening of combinatorial libraries which function by inhibiting the binding and localization of proteinase MMP2 to integrin alpha(V)beta(3).
Journal of the American Chemical Society 2001;123(7):1280-8.
2001: Dale L Boger; Satoshi Ichikawa; Winston C Tse; Michael P Hedrick; Qing Jin
Total syntheses of thiocoraline and BE-22179 and assessment of their DNA binding and biological properties.
Journal of the American Chemical Society 2001;123(4):561-8.
2001: Steven A. Silletti; Torsten Kessler; Joel Goldberg; Dale L Boger; David A Cheresh
Disruption of matrix metalloproteinase 2 binding to integrin alpha vbeta 3 by an organic molecule inhibits angiogenesis and tumor growth in vivo.
Proceedings of the National Academy of Sciences of the United States of America 2001;98(1):119-24.
2000: Dale L Boger; Scott E Wolkenberg
Total synthesis of Amaryllidaceae alkaloids utilizing sequential intramolecular heterocyclic azadiene Diels-Alder reactions of an unsymmetrical 1,2,4,5-tetrazine.
The Journal of organic chemistry 2000;65(26):9120-4.
2000: Dale L Boger; Robert A Fecik; JE Patterson; Hiroshi Miyauchi; Matthew P Patricelli; Benjamin F Cravatt
Fatty acid amide hydrolase substrate specificity.
Bioorganic & medicinal chemistry letters 2000;10(23):2613-6.
2000: Dale L Boger; Richard J Lee; Pierre-Yves Bounaud; P Meier
Asymmetric synthesis of orthogonally protected L-threo-beta-hydroxyasparagine.
The Journal of organic chemistry 2000;65(20):6770-2.
2000: Dale L Boger; J K Lee
Development of a solution-phase synthesis of minor groove binding bis-intercalators based on triostin A suitable for combinatorial synthesis.
The Journal of organic chemistry 2000;65(19):5996-6000.
2000: Dale L Boger; Y Chen; C A Foster
Synthesis and evaluation of aza HUN-7293.
Bioorganic & medicinal chemistry letters 2000;10(15):1741-4.
2000: Dale L Boger; M A Dechantsreiter; Takahiro Ishii; BE Fink; Michael P Hedrick
Assessment of solution-phase positional scanning libraries based on distamycin A for the discovery of new DNA binding agents.
Bioorganic & medicinal chemistry 2000;8(8):2049-57.
2000: J A Smith; G Bifulco; David A Case; Dale L Boger; Luigi Gomez-Paloma; Walter J Chazin
The structural basis for in situ activation of DNA alkylation by duocarmycin SA.
Journal of molecular biology 2000;300(5):1195-204.
2000: Dale L Boger; Thomas H Marsilje; R A Castro; Michael P Hedrick; Qing Jin; Stephen J Baker; JH Shim; Stephen J Benkovic
Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.
Bioorganic & medicinal chemistry letters 2000;10(13):1471-5.
2000: Dale L Boger; A Santillán; M Searcey; SR Brunette; Scott E Wolkenberg; Michael P Hedrick; Qing Jin
Synthesis and evaluation of 1,2,8, 8a-Tetrahydrocyclopropa[c]pyrrolo[3,2-e]indol-4(5H)-one, the parent alkylation subunit of CC-1065 and the duocarmycins: impact of the alkylation subunit substituents and its implications for DNA alkylation catalysis.
The Journal of organic chemistry 2000;65(13):4101-11.
2000: Dale L Boger; C W Boyce
Selective metal cation activation of a DNA alkylating agent: synthesis and evaluation of methyl 1,2,9, 9a-Tetrahydrocyclopropa[c]pyrido[3,2-e]indol-4-one-7-carboxylate (CPyI).
The Journal of organic chemistry 2000;65(13):4088-100.
2000: Dale L Boger; BE Fink; Michael P Hedrick
A new class of highly cytotoxic diketopiperazines.
Bioorganic & medicinal chemistry letters 2000;10(10):1019-20.
2000: Dale L Boger; H Sato; AE Lerner; Michael P Hedrick; Robert A Fecik; Hiroshi Miyauchi; G D Wilkie; B J Austin; Matthew P Patricelli; Benjamin F Cravatt
Exceptionally potent inhibitors of fatty acid amide hydrolase: the enzyme responsible for degradation of endogenous oleamide and anandamide.
Proceedings of the National Academy of Sciences of the United States of America 2000;97(10):5044-9.
2000: Dale L Boger; Marc A Labroli; Thomas H Marsilje; Qing Jin; Michael P Hedrick; Stephen J Baker; JH Shim; Stephen J Benkovic
Conformationally restricted analogues designed for selective inhibition of GAR Tfase versus thymidylate synthase or dihydrofolate reductase.
Bioorganic & medicinal chemistry 2000;8(5):1075-86.
2000: Dale L Boger; Danielle R Soenen; C W Boyce; Michael P Hedrick; Qing Jin
Total synthesis of ningalin B utilizing a heterocyclic azadiene Diels-Alder reaction and discovery of a new class of potent multidrug resistant (MDR) reversal agents.
The Journal of organic chemistry 2000;65(8):2479-83.
2000: Dale L Boger; J K Lee; Joel Goldberg; Qing Jin
Two comparisons of the performance of positional scanning and deletion synthesis for the identification of active constituents in mixture combinatorial libraries.
The Journal of organic chemistry 2000;65(5):1467-74.
2000: Dale L Boger; M Searcey; Winston C Tse; Qing Jin
Bifunctional alkylating agents derived from duocarmycin SA: potent antitumor activity with altered sequence selectivity.
Bioorganic & medicinal chemistry letters 2000;10(5):495-8.
1999: Samantha E Greasley; M M Yamashita; H Cai; Stephen J Benkovic; Dale L Boger; Ian A Wilson
New insights into inhibitor design from the crystal structure and NMR studies of Escherichia coli GAR transformylase in complex with beta-GAR and 10-formyl-5,8,10-trideazafolic acid.
Biochemistry 1999;38(51):16783-93.
1999: Pier Giovanni Baraldi; Barbara Cacciari; LUISA-CARLOTA LÓPEZ-CARA; Giampiero Spalluto; C W Boyce; Dale L Boger
Resolution of a CPzI precursor, synthesis and biological evaluation of (+) and (-)-N-Boc-CPzI: a further validation of the relationship between chemical solvolytic stability and cytotoxicity.
Bioorganic & medicinal chemistry letters 1999;9(21):3087-92.
1999: Dale L Boger; H Sato; AE Lerner; Xuen Guan; Norton B Gilula
Arachidonic acid amide inhibitors of gap junction cell-cell communication.
Bioorganic & medicinal chemistry letters 1999;9(8):1151-4.
1999: Dale L Boger; K W Saionz
DNA binding properties of key sandramycin analogues: systematic examination of the intercalation chromophore.
Bioorganic & medicinal chemistry 1999;7(2):315-21.
1999: Dale L Boger; H Sato; AE Lerner; B J Austin; JE Patterson; Matthew P Patricelli; Benjamin F Cravatt
Trifluoromethyl ketone inhibitors of fatty acid amide hydrolase: a probe of structural and conformational features contributing to inhibition.
Bioorganic & medicinal chemistry letters 1999;9(2):265-70.
1998: Dale L Boger; P Ducray; W Chai; Wanlong Jiang; Joel Goldberg
Higher order iminodiacetic acid libraries for probing protein-protein interactions.
Bioorganic & medicinal chemistry letters 1998;8(17):2339-44.
1998: Dale L Boger; Steven J Henriksen; Benjamin F Cravatt
Oleamide: an endogenous sleep-inducing lipid and prototypical member of a new class of biological signaling molecules.
Current pharmaceutical design 1998;4(4):303-14.
1998: Dale L Boger; Joel Goldberg; Wanlong Jiang; W Chai; P Ducray; J K Lee; Rachel S Ozer; C M Andersson
Higher order iminodiacetic acid libraries for probing protein-protein interactions.
Bioorganic & medicinal chemistry 1998;6(8):1347-78.
1998: Dale L Boger; M J Kochanny; H Cai; D Wyatt; Paul Kitos; MS Warren; Joseph Ramcharan; Lata T Gooljarsingh; Stephen J Benkovic
Design, synthesis, and evaluation of potential GAR and AICAR transformylase inhibitors.
Bioorganic & medicinal chemistry 1998;6(6):643-59.
1998: Dale L Boger; JE Patterson; Xuen Guan; Benjamin F Cravatt; Richard A Lerner; Norton B Gilula
Chemical requirements for inhibition of gap junction communication by the biologically active lipid oleamide.
Proceedings of the National Academy of Sciences of the United States of America 1998;95(9):4810-5.
1998: Dale L Boger; JE Patterson; Q Jin
Structural requirements for 5-HT2A and 5-HT1A serotonin receptor potentiation by the biologically active lipid oleamide.
Proceedings of the National Academy of Sciences of the United States of America 1998;95(8):4102-7.
1998: Dale L Boger; R T Beresis; O Loiseleur; J H Wu; Steven L Castle
Synthesis of the vancomycin CDE ring system.
Bioorganic & medicinal chemistry letters 1998;8(7):721-4.
1998: Matthew P Patricelli; JE Patterson; Dale L Boger; Benjamin F Cravatt
An endogenous sleep-inducing compound is a novel competitive inhibitor of fatty acid amide hydrolase.
Bioorganic & medicinal chemistry letters 1998;8(6):613-8.
1998: Dale L Boger; J H Chen; K W Saionz; Qing Jin
Synthesis of key sandramycin analogs: systematic examination of the intercalation chromophore.
Bioorganic & medicinal chemistry 1998;6(1):85-102.
1997: Xuen Guan; Benjamin F Cravatt; G R Ehring; James E Hall; Dale L Boger; Richard A Lerner; Norton B Gilula
The sleep-inducing lipid oleamide deconvolutes gap junction communication and calcium wave transmission in glial cells.
The Journal of cell biology 1997;139(7):1785-92.
1997: P S Eis; J A Smith; J M Rydzewski; David A Case; Dale L Boger; Walter J Chazin
High resolution solution structure of a DNA duplex alkylated by the antitumor agent duocarmycin SA.
Journal of molecular biology 1997;272(2):237-52.
1997: Dale L Boger; NE Haynes; MS Warren; Joseph Ramcharan; Paul Kitos; Stephen J Benkovic
Multisubstrate analogue based on 5,8,10-trideazafolate.
Bioorganic & medicinal chemistry 1997;5(9):1853-7.
1997: Dale L Boger; NE Haynes; MS Warren; Joseph Ramcharan; AE Marolewski; Paul Kitos; Stephen J Benkovic
Abenzyl 10-formyl-trideazafolic acid (abenzyl 10-formyl-TDAF): an effective inhibitor of glycinamide ribonucleotide transformylase.
Bioorganic & medicinal chemistry 1997;5(9):1847-52.
1997: Dale L Boger; NE Haynes; MS Warren; Joseph Ramcharan; Paul Kitos; Stephen J Benkovic
Functionalized analogues of 5,8,10-trideazafolate: development of an enzyme-assembled tight binding inhibitor of GAR Tfase and a potential irreversible inhibitor of AICAR Tfase.
Bioorganic & medicinal chemistry 1997;5(9):1839-46.
1997: Dale L Boger; NE Haynes; MS Warren; Lata T Gooljarsingh; Joseph Ramcharan; Paul Kitos; Stephen J Benkovic
Functionalized analogues of 5,8,10-trideazafolate as potential inhibitors of GAR Tfase or AICAR Tfase.
Bioorganic & medicinal chemistry 1997;5(9):1831-8.
1997: Dale L Boger; NE Haynes; Paul Kitos; MS Warren; Joseph Ramcharan; AE Marolewski; Stephen J Benkovic
10-Formyl-5,8,10-trideazafolic acid (10-formyl-TDAF): a potent inhibitor of glycinamide ribonucleotide transformylase.
Bioorganic & medicinal chemistry 1997;5(9):1817-30.
1997: Dale L Boger; S Teramoto; H Cai
N-methyl threonine analogues of deglycobleomycin A2: synthesis and evaluation.
Bioorganic & medicinal chemistry 1997;5(8):1577-89.
1997: Dale L Boger; R M Garbaccio
Catalysis of the CC-1065 and duocarmycin DNA alkylation reaction: DNA binding induced conformational change in the agent results in activation.
Bioorganic & medicinal chemistry 1997;5(2):263-76.
1997: Dale L Boger; N Han
CC-1065/duocarmycin and bleomycin A2 hybrid agents: lack of enhancement of DNA alkylation by attachment to noncomplementary DNA binding subunits.
Bioorganic & medicinal chemistry 1997;5(2):233-43.
1996: Benjamin F Cravatt; DK Giang; Stephen P Mayfield; Dale L Boger; Richard A Lerner; Norton B Gilula
Molecular characterization of an enzyme that degrades neuromodulatory fatty-acid amides.
Nature 1996;384(6604):83-7.
1996: Dale L Boger; J Zhou
Key analogues of the tetrapeptide subunit of RA-VII and deoxybouvardin.
Bioorganic & medicinal chemistry 1996;4(10):1597-603.
1996: Dale L Boger; J Zhou; H Cai
Demonstration and definition of the noncovalent binding selectivity of agents related to CC-1065 by an affinity cleavage agent: noncovalent binding coincidental with alkylation.
Bioorganic & medicinal chemistry 1996;4(6):859-67.
1996: S Cheng; C M Tarby; D D Comer; J P Williams; L H Caporale; P L Myers; Dale L Boger
A solution-phase strategy for the synthesis of chemical libraries containing small organic molecules: a universal and dipeptide mimetic template.
Bioorganic & medicinal chemistry 1996;4(5):727-37.
1996: Dale L Boger; T M Ramsey; H Cai
Synthesis and evaluation of potential N pi and N sigma metal chelation sites within the beta-hydroxy-L-histidine subunit of bleomycin A2: functional characterization of imidazole N pi metal complexation.
Bioorganic & medicinal chemistry 1996;4(2):195-207.
1996: Dale L Boger; S Teramoto; H Cai
Synthesis and evaluation of deglycobleomycin A2 analogues containing a tertiary N-methyl amide and simple ester replacement for the L-histidine secondary amide: direct functional characterization of the requirement for secondary amide metal complexation.
Bioorganic & medicinal chemistry 1996;4(2):179-93.
1995: Dale L Boger; J Zhou; B Winter; Paul Kitos
Key analogs of the tetrapeptide subunit of RA-VII and deoxybouvardin.
Bioorganic & medicinal chemistry 1995;3(12):1579-93.
1995: Dale L Boger; W Yun; N Han
1,2,9,9a-Tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) analogs of CC-1065 and the duocarmycins: synthesis and evaluation.
Bioorganic & medicinal chemistry 1995;3(11):1429-53.
1995: Dale L Boger; S L Colletti; S Teramoto; T M Ramsey; J Zhou
Synthesis of key analogs of bleomycin A2 that permit a systematic evaluation of the linker region: identification of an exceptionally prominent role for the L-threonine substituent.
Bioorganic & medicinal chemistry 1995;3(9):1281-95.
1995: Benjamin F Cravatt; O Prospero-Garcia; Gary Siuzdak; Norton B Gilula; Steven J Henriksen; Dale L Boger; Richard A Lerner
Chemical characterization of a family of brain lipids that induce sleep.
Science (New York, N.Y.) 1995;268(5216):1506-9.
1995: Dale L Boger; W Yun; H Cai; N Han
CBI-CDPBO1 and CBI-CDPBI1: CC-1065 analogs containing deep-seated modifications in the DNA binding subunit.
Bioorganic & medicinal chemistry 1995;3(6):761-7.
1995: Dale L Boger; W Yun; N Han; D S Johnson
CC-1065 CBI analogs: an example of enhancement of DNA alkylation efficiency through introduction of stabilizing electrostatic interactions.
Bioorganic & medicinal chemistry 1995;3(6):611-21.
1995: Dale L Boger; D S Johnson
CC-1065 and the duocarmycins: unraveling the keys to a new class of naturally derived DNA alkylating agents.
Proceedings of the National Academy of Sciences of the United States of America 1995;92(9):3642-9.
1995: Dale L Boger; T Nishi
Diastereoselective Dieckmann condensation suitable for introduction of the duocarmycin A C6 center: development of a divergent strategy for the total synthesis of duocarmycins A and SA.
Bioorganic & medicinal chemistry 1995;3(1):67-77.
1994: Richard A Lerner; Gary Siuzdak; O Prospero-Garcia; Steven J Henriksen; Dale L Boger; Benjamin F Cravatt
Cerebrodiene: a brain lipid isolated from sleep-deprived cats.
Proceedings of the National Academy of Sciences of the United States of America 1994;91(20):9505-8.
1994: Dale L Boger; M A Patane; Q Jin; Paul Kitos
Design, synthesis and evaluation of bouvardin, deoxybouvardin and RA-I-XIV pharmacophore analogs.
Bioorganic & medicinal chemistry 1994;2(2):85-100.
1994: Dale L Boger; D S Johnson; W Yun; C M Tarby
Molecular basis for sequence selective DNA alkylation by (+)- and ent-(-)-CC-1065 and related agents: alkylation site models that accommodate the offset AT-rich adenine N3 alkylation selectivity.
Bioorganic & medicinal chemistry 1994;2(2):115-35.
1994: F Mohamadi; M M Spees; G S Staten; Philip Marder; J K Kipka; D A Johnson; Dale L Boger; Hamideh Zarrinmayeh
Total synthesis and biological properties of novel antineoplastic (chloromethyl)furanoindolines: an asymmetric hydroboration mediated synthesis of the alkylation subunits.
Journal of medicinal chemistry 1994;37(2):232-9.
1993: Dale L Boger; D S Johnson; M S Palanki; Paul Kitos; J Chang; P Dowell
Evaluation of functional analogs of CC-1065 and the duocarmycins incorporating the cross-linking 9a-chloromethyl-1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-on e (C2BI) alkylation subunit.
Bioorganic & medicinal chemistry 1993;1(1):27-38.
1991: Dale L Boger; Hamideh Zarrinmayeh; S A Munk; Paul Kitos; O Suntornwat
Demonstration of a pronounced effect of noncovalent binding selectivity on the (+)-CC-1065 DNA alkylation and identification of the pharmacophore of the alkylation subunit.
Proceedings of the National Academy of Sciences of the United States of America 1991;88(4):1431-5.
1990: Dale L Boger; B J Invergo; R S Coleman; Hamideh Zarrinmayeh; Paul Kitos; S C Thompson; T Leong; L W McLaughlin
A demonstration of the intrinsic importance of stabilizing hydrophobic binding and non-covalent van der Waals contacts dominant in the non-covalent CC-1065/B-DNA binding.
Chemico-biological interactions 1990;73(1):29-52.
1987: Dale L Boger; M Yasuda; Lester A Mitscher; S D Drake; Paul Kitos; S C Thompson
Streptonigrin and lavendamycin partial structures. Probes for the minimum, potent pharmacophore of streptonigrin, lavendamycin, and synthetic quinoline-5,8-diones.
Journal of medicinal chemistry 1987;30(10):1918-28.
1985: Dale L Boger; Lester A Mitscher; M D Mullican; S D Drake; Paul Kitos
Antimicrobial and cytotoxic properties of 9,10-dihydrophenanthrenes: structure-activity studies on juncusol.
Journal of medicinal chemistry 1985;28(10):1543-7.