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George Hartman

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Vadim Y Dudkin; Mark E Fraley; Kelly Hamilton; George D Hartman; Mari Ikuta; Constantine Kreatsoulas; Robert B Lobell; Keith Rickert; Steven M Stirdivant; Eileen S Walsh; Cheng Wang; Yowei Yan; Kenneth L Arrington; Carolyn A Buser; Robert A Drakas; Laura Sepp-Lorenzino
Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates.
Vadim Y Dudkin; Mark E Fraley; Kelly Hamilton; James Hardwick; George D Hartman; Robert B Lobell; Xianzhi Mao; Keith Rickert; Kenneth L Arrington; Stephen C Beck; Carolyn A Buser; Robert A Drakas; Steven M Stirdivant; Weikang Tao; Eileen S Walsh; Cheng Wang; Laura Sepp-Lorenzino
Pyridyl aminothiazoles as potent Chk1 inhibitors: optimization of cellular activity.
Paul J Coleman; Christopher D Cox; Donghui Cui; Scott M Doran; Steven V Fox; Susan L Garson; Anthony Gotter; Charles M Harrell; George D Hartman; Wei Lemaire; Georgia B McGaughey; Thomayant Prueksaritanont; Duane R Reiss; Richard G Ball; Rodney A Bednar; Michael J Bogusky; Michael J Breslin; Tamara D Cabalu; John D Schreier; Joyce Stellabott; Joanne Stevens; Pamela L Tannenbaum; David B Whitman; Chris Winrow; Steven D Young; John Renger
Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties.

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All Publications

2012: Vadim Y Dudkin; Mark E Fraley; Kelly Hamilton; George D Hartman; Mari Ikuta; Constantine Kreatsoulas; Robert B Lobell; Keith Rickert; Steven M Stirdivant; Eileen S Walsh; Cheng Wang; Yowei Yan; Kenneth L Arrington; Carolyn A Buser; Robert A Drakas; Laura Sepp-Lorenzino
Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates.
Bioorganic & medicinal chemistry letters 2012;22(7):2609-12.
2012: Vadim Y Dudkin; Mark E Fraley; Kelly Hamilton; James Hardwick; George D Hartman; Robert B Lobell; Xianzhi Mao; Keith Rickert; Kenneth L Arrington; Stephen C Beck; Carolyn A Buser; Robert A Drakas; Steven M Stirdivant; Weikang Tao; Eileen S Walsh; Cheng Wang; Laura Sepp-Lorenzino
Pyridyl aminothiazoles as potent Chk1 inhibitors: optimization of cellular activity.
Bioorganic & medicinal chemistry letters 2012;22(7):2613-9.
2012: Paul J Coleman; Christopher D Cox; Donghui Cui; Scott M Doran; Steven V Fox; Susan L Garson; Anthony Gotter; Charles M Harrell; George D Hartman; Wei Lemaire; Georgia B McGaughey; Thomayant Prueksaritanont; Duane R Reiss; Richard G Ball; Rodney A Bednar; Michael J Bogusky; Michael J Breslin; Tamara D Cabalu; John D Schreier; Joyce Stellabott; Joanne Stevens; Pamela L Tannenbaum; David B Whitman; Chris Winrow; Steven D Young; John Renger
Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties.
ChemMedChem 2012;7(3):415-24, 337.
2011: Christopher J Bungard; Danielle H Euler; Yulin Fang; George D Hartman; James C Hershey; Jesse J Manikowski; Ryan Norcross; James J Perkins; Thomas H Rushmore; Azriel Schmidt; Charles D Thompson; Chang Bai; Philip E Brandish; Robert S Meissner
Discovery of selective glucocorticoid receptor modulator MK-5932.
Bioorganic & medicinal chemistry 2011;19(24):7374-86.
2011: Scott D Kuduk; Michael Leitl; Robert H Spencer; Mark O Urban; Matthew J Cato; Ronald K Chang; Sean P Cook; Christina N Di Marco; Robert M DiPardo; George D Hartman; Aneta Jovanovska; Stefanie A Kane; Mark T Bilodeau
Identification of non-amidine inhibitors of acid-sensing ion channel-3 (ASIC3).
Bioorganic & medicinal chemistry letters 2011;21(14):4255-8.
2011: Scott D Kuduk; Lei Ma; Daniel R Pitts; Mark T Bilodeau; Ronald K Chang; Christina N Di Marco; Thomas J Greshock; George D Hartman; Kenneth A Koeplinger; Matthew A Seager; Charles D Thompson; Marion Wittmann; William J Ray
Discovery of a selective allosteric M1 receptor modulator with suitable development properties based on a quinolizidinone carboxylic acid scaffold.
Journal of medicinal chemistry 2011;54(13):4773-80.
2011: Scott E Wolkenberg; Zhijian Zhao; James J Mulhearn; Scott T Harrison; John M Sanders; Matthew J Cato; Aneta Jovanovska; Jacqueline Panigel; Sean P Cook; Darrell A Henze; Stefanie A Kane; George D Hartman; James C Barrow
High concentration electrophysiology-based fragment screen: discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors.
Bioorganic & medicinal chemistry letters 2011;21(9):2646-9.
2011: Scott D Kuduk; Christina N Di Marco; Victoria Cofre; William J Ray; Lei Ma; Marion Wittmann; Matthew A Seager; Kenneth A Koeplinger; Charles D Thompson; George D Hartman; Mark T Bilodeau
Fused heterocyclic M1 positive allosteric modulators.
Bioorganic & medicinal chemistry letters 2011;21(9):2769-72.
2011: B Wesley Trotter; Kausik K Nanda; Christopher S Burgey; Craig M Potteiger; James Z Deng; Ahren I Green; John C Hartnett; Nathan R Kett; Zhicai Wu; Darrell A Henze; Kimberly Della Penna; Reshma Desai; Michael D Leitl; Wei Lemaire; Rebecca B White; Suzie Yeh; Mark O Urban; Stefanie A Kane; George D Hartman; Mark T Bilodeau
Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy.
Bioorganic & medicinal chemistry letters 2011;21(8):2354-8.
2011: Peter J Manley; Amy Zartman; Daniel V Paone; Christopher S Burgey; Darrell A Henze; Kimberly Della Penna; Reshma Desai; Michael D Leitl; Wei Lemaire; Rebecca B White; Suzie Yeh; Mark O Urban; Stefanie A Kane; George D Hartman; Mark T Bilodeau; B Wesley Trotter
Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia.
Bioorganic & medicinal chemistry letters 2011;21(8):2359-64.
2011: Scott E Wolkenberg; Zhijian Zhao; Catherine Thut; Jill W Maxwell; Terrence P McDonald; Fumi Kinose; Michael Reilly; Craig W Lindsley; George D Hartman
Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2.
Journal of medicinal chemistry 2011;54(7):2351-8.
2011: Scott D Kuduk; Ronald K Chang; Christina N Di Marco; William J Ray; Lei Ma; Marion Wittmann; Matthew A Seager; Kenneth A Koeplinger; Charles D Thompson; George D Hartman; Mark T Bilodeau
Quinolizidinone carboxylic acid selective M1 allosteric modulators: SAR in the piperidine series.
Bioorganic & medicinal chemistry letters 2011;21(6):1710-5.
2011: Thomas S Reger; Zhi-Qiang Yang; Kelly-Ann S Schlegel; Youheng Shu; Christa Mattern; Rowena V Cube; Kenneth E Rittle; Georgia B McGaughey; George D Hartman; Cuyue Tang; Jeanine Ballard; Yuhsin Kuo; Thomayant Prueksaritanont; Cindy E Nuss; Scott M Doran; Steven V Fox; Susan L Garson; Yuxing Li; Richard L Kraus; Victor N Uebele; John Renger; James C Barrow
Pyridyl amides as potent inhibitors of T-type calcium channels.
Bioorganic & medicinal chemistry letters 2011;21(6):1692-6.
2010: Kelly-Ann S Schlegel; Zhi-Qiang Yang; Thomas S Reger; Youheng Shu; Rowena Cube; Kenneth E Rittle; Phung Bondiskey; Mark G Bock; George D Hartman; Cuyue Tang; Jeanine Ballard; Yuhsin Kuo; Thomayant Prueksaritanont; Cindy E Nuss; Scott M Doran; Steven V Fox; Susan L Garson; Richard L Kraus; Yuxing Li; Victor N Uebele; John Renger; James C Barrow
Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists.
Bioorganic & medicinal chemistry letters 2010;20(17):5147-52.
2010: B Wesley Trotter; Kausik K Nanda; Peter J Manley; Victor N Uebele; Cindra L Condra; Anthony Gotter; Karsten Menzel; Martin Henault; Rino Stocco; John Renger; George D Hartman; Mark T Bilodeau
Tricyclic imidazole antagonists of the Neuropeptide S Receptor.
Bioorganic & medicinal chemistry letters 2010;20(15):4704-8.
2010: Jeffrey Y Melamed; Amy E Zartman; Nathan R Kett; Anthony Gotter; Victor N Uebele; Duane R Reiss; Cindra L Condra; Christine Fandozzi; Laura S Lubbers; Blake A Rowe; Georgia B McGaughey; Martin Henault; Rino Stocco; John Renger; George D Hartman; Mark T Bilodeau; B Wesley Trotter
Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists.
Bioorganic & medicinal chemistry letters 2010;20(15):4700-3.
2010: Christopher D Cox; Michael J Breslin; David B Whitman; John D Schreier; Georgia B McGaughey; Michael J Bogusky; Anthony J Roecker; Swati P Mercer; Rodney A Bednar; Wei Lemaire; Joseph G Bruno; Duane R Reiss; Charles M Harrell; Kathy L Murphy; Susan L Garson; Scott M Doran; Thomayant Prueksaritanont; Wayne B Anderson; Cuyue Tang; Shane Roller; Tamara D Cabalu; Donghui Cui; George D Hartman; Steven D Young; Kenneth S Koblan; Chris Winrow; John Renger; Paul J Coleman
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.
Journal of medicinal chemistry 2010;53(14):5320-32.
2010: Paul J Coleman; John D Schreier; Anthony J Roecker; Swati P Mercer; Georgia B McGaughey; Christopher D Cox; George D Hartman; Charles M Harrell; Duane R Reiss; Scott M Doran; Susan L Garson; Wayne B Anderson; Cuyue Tang; Thomayant Prueksaritanont; Chris Winrow; John Renger
Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.
Bioorganic & medicinal chemistry letters 2010;20(14):4201-5.
2010: Azriel Schmidt; Donald B Kimmel; Chang Bai; Angela Scafonas; Sujane Rutledge; Robert L Vogel; Sheila McElwee-Witmer; Fang Chen; Pascale V Nantermet; Viera Kasparcova; Chih-Tai Leu; Hai-Zhuan Zhang; Mark E Duggan; Michael A Gentile; Paul Hodor; Brenda Pennypacker; Patricia Masarachia; Evan E Opas; Sharon A Adamski; Tara E Cusick; Jiabing Wang; Helen J Mitchell; Yuntae Kim; Thomayant Prueksaritanont; James J Perkins; Robert S Meissner; George D Hartman; Leonard P Freedman; Shun-Ichi Harada; William Ray
Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology.
The Journal of biological chemistry 2010;285(22):17054-64.
2010: Edward J Brnardic; Mark E Fraley; Robert M Garbaccio; Mark E Layton; John M Sanders; Chris Culberson; Marlene A Jacobson; Brian C Magliaro; Pete H Hutson; Julie A O'Brien; Sarah L Huszar; Jason M Uslaner; Kerry L Fillgrove; Cuyue Tang; Yuhsin Kuo; Sylvie M Sur; George D Hartman
3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.
Bioorganic & medicinal chemistry letters 2010;20(10):3129-33.
2010: Chunze Li; Bing Lu; Robert M Garbaccio; Edward S Tasber; Mark E Fraley; George D Hartman; Jingjing Ye; Jane C Harrelson; Thomayant Prueksaritanont
Stereospecific reduction of a potent kinesin spindle protein (KSP) inhibitor in human tissues.
Biochemical pharmacology 2010;79(10):1526-33.
2010: Scott D Kuduk; Robert M DiPardo; Douglas C Beshore; William J Ray; Lei Ma; Marion Wittmann; Matthew A Seager; Kenneth A Koeplinger; Charles D Thompson; George D Hartman; Mark T Bilodeau
Hydroxy cycloalkyl fused pyridone carboxylic acid M(1) positive allosteric modulators.
Bioorganic & medicinal chemistry letters 2010;20(8):2538-41.
2010: Douglas C Beshore; Nigel J Liverton; Charles J McIntyre; Christopher F Claiborne; Brian E Libby; J Christopher Culberson; Joseph J Salata; Christopher P Regan; Joseph J Lynch; Laszlo Kiss; Robert H Spencer; Stefanie A Kane; Rebecca B White; Suzie Yeh; George D Hartman; Christopher Dinsmore
Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel.
Bioorganic & medicinal chemistry letters 2010;20(8):2493-6.
2010: Scott D Kuduk; Christina N Di Marco; Ronald K Chang; William J Ray; Lei Ma; Marion Wittmann; Matthew A Seager; Kenneth A Koeplinger; Charles D Thompson; George D Hartman; Mark T Bilodeau
Heterocyclic fused pyridone carboxylic acid M(1) positive allosteric modulators.
Bioorganic & medicinal chemistry letters 2010;20(8):2533-7.
2010: Paul J Coleman; John D Schreier; Georgia B McGaughey; Michael J Bogusky; Christopher D Cox; George D Hartman; Richard G Ball; Charles M Harrell; Duane R Reiss; Thomayant Prueksaritanont; Chris Winrow; John Renger
Design and synthesis of conformationally constrained N,N-disubstituted 1,4-diazepanes as potent orexin receptor antagonists.
Bioorganic & medicinal chemistry letters 2010;20(7):2311-5.
2010: Scott D Kuduk; Christina N Di Marco; Victoria Cofre; Daniel R Pitts; William J Ray; Lei Ma; Marion Wittmann; Lone Veng; Matthew A Seager; Kenneth Koeplinger; Charles D Thompson; George D Hartman; Mark T Bilodeau
N-heterocyclic derived M1 positive allosteric modulators.
Bioorganic & medicinal chemistry letters 2010;20(4):1334-7.
2010: Scott D Kuduk; Michael Leitl; Annie Liang; Nova Sain; Robert H Spencer; Mark O Urban; Vera Bodmer-Narkevitch; Matthew J Cato; Sean P Cook; Christina N Di Marco; George D Hartman; Aneta Jovanovska; Stefanie A Kane; Mark T Bilodeau
Synthesis, structure-activity relationship, and pharmacological profile of analogs of the ASIC-3 inhibitor A-317567.
ACS chemical neuroscience 2010;1(1):19-24.
2010: Feng V Yang; William D Shipe; Jaime L Bunda; M Brad Nolt; David D Wisnoski; Zhijian Zhao; James C Barrow; William J Ray; Lei Ma; Marion Wittmann; Matthew A Seager; Kenneth A Koeplinger; George D Hartman; Craig W Lindsley
Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.
Bioorganic & medicinal chemistry letters 2010;20(2):531-6.
2010: Scott D Kuduk; Christina N Di Marco; Victoria Cofre; Daniel R Pitts; William J Ray; Lei Ma; Marion Wittmann; Matthew A Seager; Matthew Seager; Kenneth Koeplinger; Charles D Thompson; George D Hartman; Mark T Bilodeau
Pyridine containing M(1) positive allosteric modulators with reduced plasma protein binding.
Bioorganic & medicinal chemistry letters 2010;20(2):657-61.
2009: Azriel Schmidt; Shun-Ichi Harada; Donald B Kimmel; Chang Bai; Fang Chen; Su Jane Rutledge; Robert L Vogel; Angela Scafonas; Michael A Gentile; Pascale V Nantermet; Sheila McElwee-Witmer; Brenda Pennypacker; Patricia Masarachia; Soumya P Sahoo; Yuntae Kim; Robert S Meissner; George D Hartman; Mark E Duggan; Gideon A Rodan; Dwight A Towler; William Ray
Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands.
The Journal of biological chemistry 2009;284(52):36367-76.
2009: Helen J Mitchell; William P Dankulich; George D Hartman; Thomayant Prueksaritanont; Azriel Schmidt; Robert L Vogel; Chang Bai; Sheila McElwee-Witmer; Hai Z Zhang; Fang Chen; Chih-Tai Leu; Donald B Kimmel; William Ray; Philippe G Nantermet; Michael A Gentile; Mark E Duggan; Robert S Meissner
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).
Journal of medicinal chemistry 2009;52(15):4578-81.
2009: Scott D Kuduk; Ronald K Chang; Jenny M-C Wai; Christina N Di Marco; Victoria Cofre; Robert M DiPardo; Sean P Cook; Matthew J Cato; Aneta Jovanovska; Mark O Urban; Michael Leitl; Robert H Spencer; Stefanie A Kane; George D Hartman; Mark T Bilodeau
Amidine derived inhibitors of acid-sensing ion channel-3 (ASIC3).
Bioorganic & medicinal chemistry letters 2009;19(15):4059-63.
2009: David B Whitman; Christopher D Cox; Michael J Breslin; Karen M Brashear; John D Schreier; Michael J Bogusky; Rodney A Bednar; Wei Lemaire; Joseph G Bruno; George D Hartman; Duane R Reiss; C Meacham Harrell; Richard L Kraus; Yuxing Li; Susan L Garson; Scott M Doran; Thomayant Prueksaritanont; Chunze Li; Chris Winrow; Kenneth S Koblan; John Renger; Paul J Coleman
Discovery of a potent, CNS-penetrant orexin receptor antagonist based on an n,n-disubstituted-1,4-diazepane scaffold that promotes sleep in rats.
ChemMedChem 2009;4(7):1069-74.
2009: Scott D Kuduk; Christina N Di Marco; Ronald K Chang; Robert M DiPardo; Sean P Cook; Matthew J Cato; Aneta Jovanovska; Mark O Urban; Michael Leitl; Robert H Spencer; Stefanie A Kane; Mark T Bilodeau; George D Hartman; Mark G Bock
Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3).
Bioorganic & medicinal chemistry letters 2009;19(9):2514-8.
2009: Scott E Wolkenberg; Zhijian Zhao; David D Wisnoski; William H Leister; Julie O'Brien; Wei Lemaire; David L Williams; Marlene A Jacobson; Cyrille Sur; Gene G Kinney; Douglas J Pettibone; Philip R Tiller; Sheri Smith; Christopher Gibson; Bennett K Ma; Stacey L Polsky-Fisher; Craig W Lindsley; George D Hartman
Discovery of GlyT1 inhibitors with improved pharmacokinetic properties.
Bioorganic & medicinal chemistry letters 2009;19(5):1492-5.
2009: Zhijian Zhao; William H Leister; Julie A O'Brien; Wei Lemaire; David L Williams; Marlene A Jacobson; Cyrille Sur; Gene G Kinney; Douglas J Pettibone; Philip R Tiller; Sheri Smith; George D Hartman; Craig W Lindsley; Scott E Wolkenberg
Discovery of N-{[1-(propylsulfonyl)-4-pyridin-2-ylpiperidin-4-yl]methyl}benzamides as novel, selective and potent GlyT1 inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(5):1488-91.
2009: Antonella Converso; Timothy Hartingh; Robert M Garbaccio; Edward Tasber; Keith Rickert; Mark E Fraley; Youwei Yan; Constantine Kreatsoulas; Steven M Stirdivant; Bob A Drakas; Eileen S Walsh; Kelly Hamilton; Carolyn A Buser; Xianzhi Mao; Marc T Abrams; Stephen C Beck; Weikang Tao; Robert B Lobell; Laura Sepp-Lorenzino; Joan Zugay-Murphy; Vinod Sardana; Sanjeev Munshi; Sylvie Marie Jezequel-Sur; Paul Zuck; George D Hartman
Development of thioquinazolinones, allosteric Chk1 kinase inhibitors.
Bioorganic & medicinal chemistry letters 2009;19(4):1240-4.
2008: Christopher D Cox; Paul J Coleman; Michael J Breslin; David B Whitman; Robert M Garbaccio; Mark E Fraley; Carolyn A Buser; Eileen S Walsh; Kelly Hamilton; Michael D Schaber; Robert B Lobell; Weikang Tao; Joseph P Davide; Ronald E Diehl; Marc T Abrams; Vicki J South; Hans E Huber; Maricel Torrent; Thomayant Prueksaritanont; Chunze Li; Donald E Slaughter; Elizabeth A Mahan; Carmen Fernandez-Metzler; Youwei Yan; Lawrence C Kuo; Nancy E Kohl; George D Hartman
Kinesin spindle protein (KSP) inhibitors. 9. Discovery of (2S)-4-(2,5-difluorophenyl)-n-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the treatment of taxane-refractory cancer.
Journal of medicinal chemistry 2008;51(14):4239-52.
2008: William D Shipe; James C Barrow; Zhi-Qiang Yang; Craig W Lindsley; F Vivien Yang; Kelly-Ann S Schlegel; Youheng Shu; Kenneth E Rittle; Mark G Bock; George D Hartman; Cuyue Tang; Jeanine E Ballard; Yuhsin Kuo; Emily D Adarayan; Thomayant Prueksaritanont; Matthew M Zrada; Victor N Uebele; Cindy E Nuss; Thomas M Connolly; Scott M Doran; Steven V Fox; Richard L Kraus; Michael J Marino; Valerie Kuzmick Graufelds; Hugo M Vargas; Patricia B Bunting; Martha Hasbun-Manning; Rose M Evans; Kenneth S Koblan; John Renger
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
Journal of medicinal chemistry 2008;51(13):3692-5.
2008: Mark T Bilodeau; Adrienne E Balitza; Jacob M Hoffman; Peter J Manley; Stanley Barnett; Deborah DeFeo-Jones; Kathleen Haskell; Raymond E Jones; Karen Leander; Ronald G Robinson; Anthony M Smith; Hans E Huber; George D Hartman
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.
Bioorganic & medicinal chemistry letters 2008;18(11):3178-82.
2008: Zhicai Wu; Ronald G Robinson; Sheng Fu; Stanley Barnett; Deborah DeFeo-Jones; Raymond E Jones; Astrid M Kral; Hans E Huber; Nancy E Kohl; George D Hartman; Mark T Bilodeau
Rapid assembly of diverse and potent allosteric Akt inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(6):2211-4.
2008: John C Hartnett; Stanley Barnett; Mark T Bilodeau; Deborah DeFeo-Jones; George D Hartman; Hans E Huber; Raymond E Jones; Astrid M Kral; Ronald G Robinson; Zhicai Wu
Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(6):2194-7.
2008: Zhicai Wu; John C Hartnett; Lou Anne Neilson; Ronald G Robinson; Sheng Fu; Stanley Barnett; Deborah DeFeo-Jones; Raymond E Jones; Astrid M Kral; Hans E Huber; George D Hartman; Mark T Bilodeau
Development of pyridopyrimidines as potent Akt1/2 inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(4):1274-9.
2008: Jeffrey M Bergman; Anthony J Roecker; Swati P Mercer; Rodney A Bednar; Duane R Reiss; Richard W Ransom; C Meacham Harrell; Douglas J Pettibone; Wei Lemaire; Kathy L Murphy; Chunze Li; Thomayant Prueksaritanont; Chris Winrow; John Renger; Kenneth S Koblan; George D Hartman; Paul J Coleman
Proline bis-amides as potent dual orexin receptor antagonists.
Bioorganic & medicinal chemistry letters 2008;18(4):1425-30.
2008: Zhijian Zhao; Scott E Wolkenberg; Philip E J Sanderson; Meiqing Lu; Vandna Munshi; Gregory Moyer; Meizhen Feng; Anthony V Carella; Linda T Ecto; Lori Gabryelski; Ming-Tain Lai; Sridar G Prasad; Youwei Yan; Georgia B McGaughey; Michael D Miller; Craig W Lindsley; George D Hartman; Joseph P Vacca; Theresa M Williams
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).
Bioorganic & medicinal chemistry letters 2008;18(2):554-9.
2008: Zhijian Zhao; Ronald G Robinson; Stanley Barnett; Deborah DeFeo-Jones; Raymond E Jones; George D Hartman; Hans E Huber; Mark E Duggan; Craig W Lindsley
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.
Bioorganic & medicinal chemistry letters 2008;18(1):49-53.
2007: Robert M Garbaccio; Shaei Huang; Edward S Tasber; Mark E Fraley; Youwei Yan; Sanjeev Munshi; Mari Ikuta; Lawrence Kuo; Constantine Kreatsoulas; Steven M Stirdivant; Bob A Drakas; Keith Rickert; Eileen S Walsh; Kelly A Hamilton; Carolyn A Buser; James Hardwick; Xianzhi Mao; Stephen C Beck; Marc T Abrams; Weikang Tao; Robert B Lobell; Laura Sepp-Lorenzino; George D Hartman
Synthesis and evaluation of substituted benzoisoquinolinones as potent inhibitors of Chk1 kinase.
Bioorganic & medicinal chemistry letters 2007;17(22):6280-5.
2007: Edward J Brnardic; Robert M Garbaccio; Mark E Fraley; Edward S Tasber; Justin T Steen; Kenneth L Arrington; Vadim Y Dudkin; George D Hartman; Steven M Stirdivant; Bob A Drakas; Keith Rickert; Eileen S Walsh; Kelly Hamilton; Carolyn A Buser; James Hardwick; Weikang Tao; Stephen C Beck; Xianzhi Mao; Robert B Lobell; Laura Sepp-Lorenzino; Youwei Yan; Mari Ikuta; Sanjeev Munshi; Lawrence C Kuo; Constantine Kreatsoulas
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.
Bioorganic & medicinal chemistry letters 2007;17(21):5989-94.
2007: Robert M Garbaccio; Edward S Tasber; Lou Anne Neilson; Paul J Coleman; Mark E Fraley; Christy Olson; Jeff Bergman; Maricel Torrent; Carolyn A Buser; Keith Rickert; Eileen S Walsh; Kelly Hamilton; Robert B Lobell; Weikang Tao; Vicki J South; Ronald E Diehl; Joseph P Davide; Youwei Yan; Lawrence C Kuo; Chunze Li; Thomayant Prueksaritanont; Carmen Fernandez-Metzler; Elizabeth A Mahan; Donald E Slaughter; Joseph J Salata; Nancy E Kohl; Hans E Huber; George D Hartman
Kinesin spindle protein (KSP) inhibitors. Part 7: Design and synthesis of 3,3-disubstituted dihydropyrazolobenzoxazines as potent inhibitors of the mitotic kinesin KSP.
Bioorganic & medicinal chemistry letters 2007;17(20):5671-6.
2007: Anthony J Roecker; Paul J Coleman; Swati P Mercer; John D Schreier; Carolyn A Buser; Eileen S Walsh; Kelly Hamilton; Robert B Lobell; Weikang Tao; Ronald E Diehl; Vicki J South; Joseph P Davide; Nancy E Kohl; Youwei Yan; Lawrence C Kuo; Chunze Li; Carmen Fernandez-Metzler; Elizabeth A Mahan; Thomayant Prueksaritanont; George D Hartman
Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP.
Bioorganic & medicinal chemistry letters 2007;17(20):5677-82.
2007: Paul J Coleman; John D Schreier; Christopher D Cox; Mark E Fraley; Robert M Garbaccio; Carolyn A Buser; Eileen S Walsh; Kelly Hamilton; Robert B Lobell; Keith Rickert; Weikang Tao; Ronald E Diehl; Vicki J South; Joseph P Davide; Nancy E Kohl; Youwei Yan; Lawrence Kuo; Thomayant Prueksaritanont; Chunze Li; Elizabeth A Mahan; Carmen Fernandez-Metzler; Joseph J Salata; George D Hartman
Kinesin spindle protein (KSP) inhibitors. Part 6: Design and synthesis of 3,5-diaryl-4,5-dihydropyrazole amides as potent inhibitors of the mitotic kinesin KSP.
Bioorganic & medicinal chemistry letters 2007;17(19):5390-5.
2007: Christopher D Cox; Michael J Breslin; David B Whitman; Paul J Coleman; Robert M Garbaccio; Mark E Fraley; Matthew M Zrada; Carolyn A Buser; Eileen S Walsh; Kelly Hamilton; Robert B Lobell; Weikang Tao; Marc T Abrams; Vicki J South; Hans E Huber; Nancy E Kohl; George D Hartman
Kinesin spindle protein (KSP) inhibitors. Part V: discovery of 2-propylamino-2,4-diaryl-2,5-dihydropyrroles as potent, water-soluble KSP inhibitors, and modulation of their basicity by beta-fluorination to overcome cellular efflux by P-glycoprotein.
Bioorganic & medicinal chemistry letters 2007;17(10):2697-702.
2007: Zhijian Zhao; David D Wisnoski; Julie A O'Brien; Wei Lemaire; David L Williams; Marlene A Jacobson; Marion Wittman; Sookhee N Ha; Hervé Schaffhauser; Cyrille Sur; Douglas J Pettibone; Mark E Duggan; P Jeffrey Conn; George D Hartman; Craig W Lindsley
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Bioorganic & medicinal chemistry letters 2007;17(5):1386-91.
2006: Zhijian Zhao; Julie A O'Brien; Wei Lemaire; David L Williams; Marlene A Jacobson; Cyrille Sur; Douglas J Pettibone; Philip R Tiller; Sheri Smith; George D Hartman; Scott E Wolkenberg; Craig W Lindsley
Synthesis and SAR of GlyT1 inhibitors derived from a series of N-((4-(morpholine-4-carbonyl)-1-(propylsulfonyl)piperidin-4-yl)methyl)benzamides.
Bioorganic & medicinal chemistry letters 2006;16(23):5968-72.
2006: Mark E Fraley; Justin T Steen; Edward J Brnardic; Kenneth L Arrington; Keith L Spencer; Barbara A Hanney; Yuntae Kim; George D Hartman; Steven M Stirdivant; Bob A Drakas; Keith Rickert; Eileen S Walsh; Kelly Hamilton; Carolyn A Buser; James Hardwick; Weikang Tao; Stephen C Beck; Xianzhi Mao; Robert B Lobell; Laura Sepp-Lorenzino; Youwei Yan; Mari Ikuta; Sanjeev Munshi; Lawrence C Kuo; Constantine Kreatsoulas
3-(Indol-2-yl)indazoles as Chek1 kinase inhibitors: Optimization of potency and selectivity via substitution at C6.
Bioorganic & medicinal chemistry letters 2006;16(23):6049-53.
2006: Wes Trotter; Kausik K Nanda; Nathan R Kett; christopher regan; Joseph J Lynch; Gary L Stump; Laszlo Kiss; Jixin Wang; Robert H Spencer; Stefanie A Kane; Rebecca B White; Rena Zhang; Kenneth D Anderson; Nigel J Liverton; Charles J McIntyre; Douglas C Beshore; George D Hartman; Christopher Dinsmore
Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation.
Journal of medicinal chemistry 2006;49(24):6954-7.
2006: Kausik K Nanda; M Brad Nolt; Matthew J Cato; Stefanie A Kane; Laszlo Kiss; Robert H Spencer; Jixin Wang; Joseph J Lynch; christopher regan; Gary L Stump; Bing Li; Rebecca White; Suzie Yeh; Michael J Bogusky; Mark T Bilodeau; Christopher Dinsmore; Craig W Lindsley; George D Hartman; Scott E Wolkenberg; Wes Trotter
Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.
Bioorganic & medicinal chemistry letters 2006;16(22):5897-901.
2006: Scott E Wolkenberg; Zhijian Zhao; Marianna Kapitskaya; Andrea L Webber; Konstantin Petrukhin; Yui S Tang; Dennis C Dean; George D Hartman; Craig W Lindsley
Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand.
Bioorganic & medicinal chemistry letters 2006;16(19):5001-4.
2006: Craig W Lindsley; Zhijian Zhao; William H Leister; Julie O'Brien; Wei Lemaire; David L Williams; Tsing-Bau Chen; Raymond S L Chang; Maryann Burno; Marlene A Jacobson; Cyrille Sur; Gene G Kinney; Douglas J Pettibone; Philip R Tiller; Sheri Smith; Nancy N Tsou; Mark E Duggan; P Jeffrey Conn; George D Hartman
Design, synthesis, and in vivo efficacy of glycine transporter-1 (GlyT1) inhibitors derived from a series of [4-phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl benzamides.
ChemMedChem 2006;1(8):807-11.
2006: Christopher D Cox; Maricel Torrent; Michael J Breslin; Brenda J Mariano; David B Whitman; Paul J Coleman; Carolyn A Buser; Eileen S Walsh; Kelly Hamilton; Michael D Schaber; Robert B Lobell; Weikang Tao; Vicki J South; Nancy E Kohl; Youwei Yan; Lawrence C Kuo; Thomayant Prueksaritanont; Donald E Slaughter; Chunze Li; Elizabeth A Mahan; Bing Lu; George D Hartman
Kinesin spindle protein (KSP) inhibitors. Part 4: Structure-based design of 5-alkylamino-3,5-diaryl-4,5-dihydropyrazoles as potent, water-soluble inhibitors of the mitotic kinesin KSP.
Bioorganic & medicinal chemistry letters 2006;16(12):3175-9.
2006: Mark E Fraley; Robert M Garbaccio; Kenneth L Arrington; William F Hoffman; Edward S Tasber; Paul J Coleman; Carolyn A Buser; Eileen S Walsh; Kelly Hamilton; Christine Fernandes; Michael D Schaber; Robert B Lobell; Weikang Tao; Vicki J South; Youwei Yan; Lawrence C Kuo; Thomayant Prueksaritanont; Cathy Shu; Maricel Torrent; David C Heimbrook; Nancy E Kohl; Hans E Huber; George D Hartman
Kinesin spindle protein (KSP) inhibitors. Part 2: the design, synthesis, and characterization of 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP.
Bioorganic & medicinal chemistry letters 2006;16(7):1775-9.
2006: Robert M Garbaccio; Mark E Fraley; Edward S Tasber; Christy M Olson; William F Hoffman; Kenneth L Arrington; Maricel Torrent; Carolyn A Buser; Eileen S Walsh; Kelly Hamilton; Michael D Schaber; Christine Fernandes; Robert B Lobell; Weikang Tao; Vicki J South; Youwei Yan; Lawrence C Kuo; Thomayant Prueksaritanont; Donald E Slaughter; Cathy Shu; David C Heimbrook; Nancy E Kohl; Hans E Huber; George D Hartman
Kinesin spindle protein (KSP) inhibitors. Part 3: synthesis and evaluation of phenolic 2,4-diaryl-2,5-dihydropyrroles with reduced hERG binding and employment of a phosphate prodrug strategy for aqueous solubility.
Bioorganic & medicinal chemistry letters 2006;16(7):1780-3.
2006: John T Sisko; Thomas J Tucker; Mark T Bilodeau; Carolyn A Buser; Patrice A Ciecko; Kathleen E Coll; Christine Fernandes; Jackson B Gibbs; Timothy J Koester; Nancy E Kohl; Joseph J Lynch; Xianzhi Mao; Debra McLoughlin; Cynthia Miller-Stein; Leonard D Rodman; Keith Rickert; Laura Sepp-Lorenzino; Jennifer M Shipman; Kenneth Thomas; Bradley K Wong; George D Hartman
Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.
Bioorganic & medicinal chemistry letters 2006;16(5):1146-50.
2005: Christopher D Cox; Michael J Breslin; Brenda J Mariano; Paul J Coleman; Carolyn A Buser; Eileen S Walsh; Kelly Hamilton; Hans E Huber; Nancy E Kohl; Maricel Torrent; Youwei Yan; Lawrence C Kuo; George D Hartman
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
Bioorganic & medicinal chemistry letters 2005;15(8):2041-5.
2005: Amy E Zartman; Le T Duong; Carmen Fernandez-Metzler; George D Hartman; Chih-Tai Leu; Thomayant Prueksaritanont; Gideon A Rodan; Sevgi B Rodan; Mark E Duggan; Robert S Meissner
Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics.
Bioorganic & medicinal chemistry letters 2005;15(6):1647-50.
2005: Zhijian Zhao; William H Leister; Ronald G Robinson; Stanley Barnett; Deborah DeFeo-Jones; Raymond E Jones; George D Hartman; Joel R Huff; Hans E Huber; Mark E Duggan; Craig W Lindsley
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(4):905-9.
2005: Craig W Lindsley; Zhijian Zhao; William H Leister; Ronald G Robinson; Stanley Barnett; Deborah DeFeo-Jones; Raymond E Jones; George D Hartman; Joel R Huff; Hans E Huber; Mark E Duggan
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
Bioorganic & medicinal chemistry letters 2005;15(3):761-4.
2004: Mark T Bilodeau; Adrienne E Balitza; Timothy J Koester; Peter J Manley; Leonard D Rodman; Carolyn Buser-Doepner; Kathleen E Coll; Christine Fernandes; Jackson B Gibbs; David C Heimbrook; William R Huckle; Nancy E Kohl; Joseph J Lynch; Xianzhi Mao; Rosemary C McFall; Debra McLoughlin; Cynthia Miller-Stein; Keith Rickert; Laura Sepp-Lorenzino; Jennifer M Shipman; Raju Subramanian; Kenneth Thomas; Bradley K Wong; Sean Yu; George D Hartman
Potent N-(1,3-thiazol-2-yl)pyridin-2-amine vascular endothelial growth factor receptor tyrosine kinase inhibitors with excellent pharmacokinetics and low affinity for the hERG ion channel.
Journal of medicinal chemistry 2004;47(25):6363-72.
2004: Craig W Lindsley; David D Wisnoski; William H Leister; Julie A O'Brien; Wei Lemaire; David L Williams; Maryann Burno; Cyrille Sur; Gene G Kinney; Douglas J Pettibone; Philip R Tiller; Sheri Smith; Mark E Duggan; George D Hartman; P Jeffrey Conn; Joel R Huff
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Journal of medicinal chemistry 2004;47(24):5825-8.
2004: Paul J Coleman; Karen M Brashear; Ben C Askew; John H Hutchinson; Carol A McVean; Le T Duong; Bradley P Feuston; Carmen Fernandez-Metzler; Michael A Gentile; George D Hartman; Donald B Kimmel; Chih-Tai Leu; Lorraine Lipfert; Kara M Merkle; Brenda Pennypacker; Thomayant Prueksaritanont; Gideon A Rodan; Gregg Wesolowski; Sevgi B Rodan; Mark E Duggan
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.
Journal of medicinal chemistry 2004;47(20):4829-37.
2004: Michael J Breslin; Mark E Duggan; Wasyl Halczenko; George D Hartman; Le T Duong; Carmen Fernandez-Metzler; Michael A Gentile; Donald B Kimmel; Chih-Tai Leu; Kara M Merkle; Thomayant Prueksaritanont; Gideon A Rodan; Sevgi B Rodan; John H Hutchinson
Nonpeptide alpha V beta 3 antagonists. Part 10: In vitro and in vivo evaluation of a potent 7-methyl substituted tetrahydro-[1,8]naphthyridine derivative.
Bioorganic & medicinal chemistry letters 2004;14(17):4515-8.
2004: David B Whitman; Ben C Askew; Le T Duong; Carmen Fernandez-Metzler; Wasyl Halczenko; George D Hartman; John H Hutchinson; Chih-Tai Leu; Thomayant Prueksaritanont; Gideon A Rodan; Sevgi B Rodan; Mark E Duggan
Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone.
Bioorganic & medicinal chemistry letters 2004;14(17):4411-5.
2004: Mark E Fraley; William F Hoffman; Kenneth L Arrington; Randall W Hungate; George D Hartman; Rosemary C McFall; Kathleen E Coll; Keith Rickert; Kenneth Thomas; Georgia B McGaughey
Property-based design of KDR kinase inhibitors.
Current medicinal chemistry 2004;11(6):709-19.
2004: Jiabing Wang; Michael J Breslin; Paul J Coleman; Mark E Duggan; Cecilia A Hunt; John H Hutchinson; Chih-Tai Leu; Sevgi B Rodan; Gideon A Rodan; Le T Duong; George D Hartman
Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.
Bioorganic & medicinal chemistry letters 2004;14(4):1049-52.
2004: Zhicai Wu; Mark E Fraley; Mark T Bilodeau; Mildred L Kaufman; Edward S Tasber; Adrienne E Balitza; George D Hartman; Kathleen E Coll; Keith Rickert; Jennifer M Shipman; Bin Shi; Laura Sepp-Lorenzino; Kenneth Thomas
Design and synthesis of 3,7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR.
Bioorganic & medicinal chemistry letters 2004;14(4):909-12.
2004: Christopher Dinsmore; C Blair Zartman; Jeffrey M Bergman; Marc T Abrams; Carolyn A Buser; J Christopher Culberson; Joseph P Davide; Michelle Ellis-Hutchings; Christine Fernandes; Samuel L Graham; George D Hartman; Hans E Huber; Robert B Lobell; Scott D Mosser; Ronald G Robinson; Theresa M Williams
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Bioorganic & medicinal chemistry letters 2004;14(3):639-43.
2004: Mark E Fraley; Kenneth L Arrington; Carolyn A Buser; Patrice A Ciecko; Kathleen E Coll; Christine Fernandes; George D Hartman; William F Hoffman; Joseph J Lynch; Rosemary C McFall; Keith Rickert; Romi Singh; Sheri Smith; Kenneth Thomas; Bradley K Wong
Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding.
Bioorganic & medicinal chemistry letters 2004;14(2):351-5.
2004: Youwei Yan; Vinod Sardana; Bei Xu; Carl F Homnick; Wasyl Halczenko; Carolyn A Buser; Michael D Schaber; George D Hartman; Hans E Huber; Lawrence C Kuo
Inhibition of a mitotic motor protein: where, how, and conformational consequences.
Journal of molecular biology 2004;335(2):547-54.
2003: James J Perkins; LT Duong; Carmen Fernandez-Metzler; George D Hartman; Donald B Kimmel; Chih-Tai Leu; Joseph J Lynch; Thomayant Prueksaritanont; Gideon A Rodan; Sevgi B Rodan; Mark E Duggan; Robert S Meissner
Non-peptide alpha(v)beta(3) antagonists: identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint.
Bioorganic & medicinal chemistry letters 2003;13(24):4285-8.
2003: Bradley P Feuston; J Christopher Culberson; George D Hartman
Molecular model of the alpha(IIb)beta(3) integrin.
Journal of medicinal chemistry 2003;46(25):5316-25.
2003: John H Hutchinson; Wasyl Halczenko; Karen M Brashear; Michael J Breslin; Paul J Coleman; Le T Duong; Carmen Fernandez-Metzler; Michael A Gentile; John E Fisher; George D Hartman; Joel R Huff; Donald B Kimmel; Chih-Tai Leu; Robert S Meissner; Kara M Merkle; Rose M Nagy; Brenda Pennypacker; James J Perkins; Thomayant Prueksaritanont; Gideon A Rodan; Sandor L Varga; Gregg Wesolowski; Amy E Zartman; Sevgi B Rodan; Mark E Duggan
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.
Journal of medicinal chemistry 2003;46(22):4790-8.
2003: Peter J Manley; Adrienne E Balitza; Mark T Bilodeau; Kathleen E Coll; George D Hartman; Rosemary C McFall; Keith Rickert; Leonard D Rodman; Kenneth Thomas
2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.
Bioorganic & medicinal chemistry letters 2003;13(10):1673-7.
2002: Bradley P Feuston; J Christopher Culberson; Mark E Duggan; George D Hartman; Chih-Tai Leu; Sevgi B Rodan
Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin.
Journal of medicinal chemistry 2002;45(26):5640-8.
2002: Karen M Brashear; Cecilia A Hunt; Brian T Kucer; Mark E Duggan; George D Hartman; Gideon A Rodan; Sevgi B Rodan; Chih-Tai Leu; Thomayant Prueksaritanont; Carmen Fernandez-Metzler; Andrea Barrish; Carl F Homnick; John H Hutchinson; Paul J Coleman
Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements.
Bioorganic & medicinal chemistry letters 2002;12(23):3483-6.
2002: Paul J Coleman; Ben C Askew; John H Hutchinson; David B Whitman; James J Perkins; George D Hartman; Gideon A Rodan; Chih-Tai Leu; Thomayant Prueksaritanont; Carmen Fernandez-Metzler; Kara M Merkle; Robert Lynch; Joseph J Lynch; Sevgi B Rodan; Mark E Duggan
Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.
Bioorganic & medicinal chemistry letters 2002;12(17):2463-5.
2002: Thomas J Tucker; Marc T Abrams; Carolyn A Buser; Joseph P Davide; Michelle Ellis-Hutchings; Christine Fernandes; Jackson B Gibbs; Samuel L Graham; George D Hartman; Hans E Huber; Dongming Liu; Robert B Lobell; William C Lumma; Ronald G Robinson; John T Sisko; Anthony M Smith
The synthesis and biological evaluation of a series of potent dual inhibitors of farnesyl and geranyl-Geranyl protein transferases.
Bioorganic & medicinal chemistry letters 2002;12(15):2027-30.
2002: George D Hartman; Mark E Fraley; Mark T Bilodeau
Kinase insert domain-containing receptor kinase inhibitors as anti-angiogenic agents.
Expert opinion on investigational drugs 2002;11(6):737-45.
2002: Paul J Coleman; Karen M Brashear; Cecilia A Hunt; William F Hoffman; John H Hutchinson; Michael J Breslin; Carol A McVean; Ben C Askew; George D Hartman; Sevgi B Rodan; Gideon A Rodan; Chih-Tai Leu; Thomayant Prueksaritanont; Carmen Fernandez-Metzler; Bennett Ma; Laura A Libby; Kara M Merkle; Gary L Stump; Audrey A Wallace; Joseph J Lynch; Robert Lynch; Mark E Duggan
Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.
Bioorganic & medicinal chemistry letters 2002;12(1):31-4.
2002: Robert S Meissner; James J Perkins; Le T Duong; George D Hartman; William F Hoffman; Joel R Huff; Nathan C Ihle; Chih-Tai Leu; Rose M Nagy; Adel M Naylor-Olsen; Gideon A Rodan; Sevgi B Rodan; David B Whitman; Gregg Wesolowski; Mark E Duggan
Nonpeptide alpha(v)beta(3) antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide.
Bioorganic & medicinal chemistry letters 2002;12(1):25-9.
2001: Robert B Lobell; CA Omer; Marc T Abrams; HG Bhimnathwala; MJ Brucker; Carolyn A Buser; Joseph P Davide; S Jane deSolms; Christopher Dinsmore; Michelle Ellis-Hutchings; AM Kral; Dongming Liu; William C Lumma; S V Machotka; Elaine Rands; Theresa M Williams; Samuel L Graham; George D Hartman; Allen Oliff; David C Heimbrook; Nancy E Kohl
Evaluation of farnesyl:protein transferase and geranylgeranyl:protein transferase inhibitor combinations in preclinical models.
Cancer research 2001;61(24):8758-68.
2001: Ian M Bell; Steven N Gallicchio; M Abrams; Douglas C Beshore; Carolyn A Buser; J Christopher Culberson; Joseph P Davide; Michelle Ellis-Hutchings; Christine Fernandes; Jackson B Gibbs; Samuel L Graham; George D Hartman; David C Heimbrook; Carl F Homnick; Joel R Huff; Kelem Kassahun; Kenneth S Koblan; Nancy E Kohl; Robert B Lobell; Joseph J Lynch; P A Miller; CA Omer; A David Rodrigues; Eileen S Walsh; Theresa M Williams
Design and biological activity of (S)-4-(5-([1-(3-chlorobenzyl)-2-oxopyrrolidin-3-ylamino]methyl)imidazol-1-ylmethyl)benzonitrile, a 3-aminopyrrolidinone farnesyltransferase inhibitor with excellent cell potency.
Journal of medicinal chemistry 2001;44(18):2933-49.
2001: Douglas C Beshore; Ian M Bell; Christopher Dinsmore; Carl F Homnick; J Christopher Culberson; Ronald G Robinson; Christine Fernandes; Eileen S Walsh; Marc T Abrams; HG Bhimnathwala; Joseph P Davide; Michelle Ellis-Hutchings; H A Huber; Kenneth S Koblan; Carolyn A Buser; Nancy E Kohl; Robert B Lobell; I-Wu Chen; Debra McLoughlin; Timothy V Olah; Samuel L Graham; George D Hartman; Theresa M Williams
Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.
Bioorganic & medicinal chemistry letters 2001;11(14):1817-21.
2001: Hans E Huber; Ronald G Robinson; A Watkins; D D Nahas; Marc T Abrams; Carolyn A Buser; Robert B Lobell; D Patrick; Neville J Anthony; Christopher Dinsmore; Samuel L Graham; George D Hartman; William C Lumma; Theresa M Williams; David C Heimbrook
Anions modulate the potency of geranylgeranyl-protein transferase I inhibitors.
The Journal of biological chemistry 2001;276(27):24457-65.
2001: Jeffrey M Bergman; Marc T Abrams; Joseph P Davide; IB Greenberg; Ronald G Robinson; Carolyn A Buser; Hans E Huber; Kenneth S Koblan; Nancy E Kohl; Robert B Lobell; Samuel L Graham; George D Hartman; Theresa M Williams; Christopher Dinsmore
Aryloxy substituted N-arylpiperazinones as dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I.
Bioorganic & medicinal chemistry letters 2001;11(11):1411-5.
2001: Christopher Dinsmore; Michael J Bogusky; J Christopher Culberson; Jeffrey M Bergman; Carl F Homnick; C Blair Zartman; Scott D Mosser; Michael D Schaber; Ronald G Robinson; Kenneth S Koblan; Hans E Huber; Samuel L Graham; George D Hartman; Joel R Huff; Theresa M Williams
Conformational restriction of flexible ligands guided by the transferred noe experiment: potent macrocyclic inhibitors of farnesyltransferase.
Journal of the American Chemical Society 2001;123(9):2107-8.
2001: Christopher Dinsmore; Jeffrey M Bergman; D D Wei; C Blair Zartman; Joseph P Davide; IB Greenberg; Dongming Liu; TJ O'Neill; Jackson B Gibbs; Kenneth S Koblan; Nancy E Kohl; Robert B Lobell; I-Wu Chen; Debra McLoughlin; Timothy V Olah; Samuel L Graham; George D Hartman; Theresa M Williams
Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.
Bioorganic & medicinal chemistry letters 2001;11(4):537-40.
2000: Mark E Duggan; LT Duong; John E Fisher; Terence G Hamill; William F Hoffman; Joel R Huff; Nathan C Ihle; Chih-Tai Leu; Rose M Nagy; James J Perkins; Sevgi B Rodan; Gregg Wesolowski; David B Whitman; Amy E Zartman; Gideon A Rodan; George D Hartman
Nonpeptide alpha(v)beta(3) antagonists. 1. Transformation of a potent, integrin-selective alpha(IIb)beta(3) antagonist into a potent alpha(v)beta(3) antagonist.
Journal of medicinal chemistry 2000;43(20):3736-45.
2000: Melissa S Egbertson; Bohumil Bednar; Ben C Askew; Rodney A Bednar; Karen M Brashear; Michael J Breslin; Mark E Duggan; Thorsten E Fisher; Wasyl Halczenko; John H Hutchinson; Nathan C Ihle; J D Prugh; John S Wai; Robert Gould; George D Hartman
Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.
Bioorganic & medicinal chemistry letters 2000;10(17):1943-8.
2000: George D Hartman; Mark E Duggan
alpha(v)beta(3) Integrin antagonists as inhibitors of bone resorption.
Expert opinion on investigational drugs 2000;9(6):1281-91.
1999: Christopher Dinsmore; Theresa M Williams; TJ O'Neill; Dongming Liu; Elaine Rands; J Christopher Culberson; Robert B Lobell; Kenneth S Koblan; Nancy E Kohl; Jackson B Gibbs; Allen Oliff; Samuel L Graham; George D Hartman
Imidazole-containing diarylether and diarylsulfone inhibitors of farnesyl-protein transferase.
Bioorganic & medicinal chemistry letters 1999;9(23):3301-6.
1999: Neville J Anthony; Robert P Gomez; Michael D Schaber; Scott D Mosser; Kelly A Hamilton; T J O'Neil; Kenneth S Koblan; Samuel L Graham; George D Hartman; D Shah; Elaine Rands; Nancy E Kohl; Jackson B Gibbs; Allen Oliff
Design and in vivo analysis of potent non-thiol inhibitors of farnesyl protein transferase.
Journal of medicinal chemistry 1999;42(17):3356-68.
1999: Terrence M Ciccarone; Suzanne C MacTough; Theresa M Williams; Christopher Dinsmore; TJ O'Neill; D Shah; J Christopher Culberson; Kenneth S Koblan; Nancy E Kohl; Jackson B Gibbs; Allen Oliff; Samuel L Graham; George D Hartman
Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.
Bioorganic & medicinal chemistry letters 1999;9(14):1991-6.
1999: Bohumil Bednar; Jacquelynn J Cook; Marie A Holahan; Michael E Cunningham; P A Jumes; Rodney A Bednar; George D Hartman; Robert Gould
Fibrinogen receptor antagonist-induced thrombocytopenia in chimpanzee and rhesus monkey associated with preexisting drug-dependent antibodies to platelet glycoprotein IIb/IIIa.
Blood 1999;94(2):587-99.
1999: Melissa S Egbertson; Jacquelynn J Cook; Bohumil Bednar; J D Prugh; Rodney A Bednar; Stanley L Gaul; Robert Gould; George D Hartman; Carl F Homnick; Marie A Holahan; L A Libby; Joseph J Lynch; RJ Lynch; Gary R Sitko; Maria T Stranieri; L M Vassallo
Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.
Journal of medicinal chemistry 1999;42(13):2409-21.
1999: George D Hartman; Mark E Duggan; William F Hoffman; R J Meissner; James J Perkins; Amy E Zartman; Adel M Naylor-Olsen; Jacquelynn J Cook; JD Glass; RJ Lynch; G Zhang; Robert Gould
Nonpeptide glycoprotein IIB/IIIA inhibitors. 19. A new design paradigm employing linearly minimized, centrally constrained, exosite inhibitors.
Bioorganic & medicinal chemistry letters 1999;9(6):863-8.
1998: Rodney A Bednar; Stanley L Gaul; Terence G Hamill; Melissa S Egbertson; Jules A Shafer; George D Hartman; Robert Gould; Bohumil Bednar
Identification of low molecular weight GP IIb/IIIa antagonists that bind preferentially to activated platelets.
The Journal of pharmacology and experimental therapeutics 1998;285(3):1317-26.
1997: Jacquelynn J Cook; JD Glass; Gary R Sitko; Marie A Holahan; R F Stupienski; Audrey A Wallace; Gary L Stump; Elizabeth Hand; Ben C Askew; George D Hartman; Robert Gould; Joseph J Lynch
Nonpeptide glycoprotein IIb/IIIa inhibitors: 14: oral antithrombotic efficacy of L-738,167 in a conscious canine model of coronary artery electrolytic injury.
Circulation 1997;96(3):949-58.
1997: Jackson B Gibbs; Samuel L Graham; George D Hartman; Kenneth S Koblan; Nancy E Kohl; CA Omer; Allen Oliff
Farnesyltransferase inhibitors versus Ras inhibitors.
Current opinion in chemical biology 1997;1(2):197-203.
1997: Thomayant Prueksaritanont; LM Gorham; Michael J Breslin; John H Hutchinson; George D Hartman; Kamlesh P Vyas; Thomas A Baillie
In vitro and in vivo evaluations of the metabolism, pharmacokinetics, and bioavailability of ester prodrugs of L-767,679, a potent fibrinogen receptor antagonist: an approach for the selection of a prodrug candidate.
Drug metabolism and disposition: the biological fate of chemicals 1997;25(8):978-84.
1997: Ben C Askew; Rodney A Bednar; Bohumil Bednar; David A Claremon; Jacquelynn J Cook; Charles J McIntyre; Cecilia A Hunt; Robert Gould; RJ Lynch; Joseph J Lynch; Stanley L Gaul; Maria T Stranieri; Gary R Sitko; Marie A Holahan; JD Glass; Terence G Hamill; LM Gorham; Thomayant Prueksaritanont; JJ Baldwin; George D Hartman
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists.
Journal of medicinal chemistry 1997;40(12):1779-88.
1997: Jacquelynn J Cook; Gary R Sitko; Marie A Holahan; Maria T Stranieri; JD Glass; Ben C Askew; Charles J McIntyre; David A Claremon; JJ Baldwin; George D Hartman; Robert Gould; Joseph J Lynch
Nonpeptide glycoprotein IIb/IIIa inhibitors. 15. Antithrombotic efficacy of L-738,167, a long-acting GPIIb/IIIa antagonist, correlates with inhibition of adenosine diphosphate-induced platelet aggregation but not with bleeding time prolongation.
The Journal of pharmacology and experimental therapeutics 1997;281(2):677-89.
1997: Bohumil Bednar; Michael E Cunningham; P A McQueney; Melissa S Egbertson; Ben C Askew; Rodney A Bednar; George D Hartman; Robert Gould
Flow cytometric measurement of kinetic and equilibrium binding parameters of arginine-glycine-aspartic acid ligands in binding to glycoprotein IIb/IIIa on platelets.
Cytometry 1997;28(1):58-65.
1997: CA Omer; Neville J Anthony; Carolyn Buser-Doepner; A L Burkhardt; S Jane deSolms; Christopher Dinsmore; Jackson B Gibbs; George D Hartman; Kenneth S Koblan; Robert B Lobell; Allen Oliff; Theresa M Williams; Nancy E Kohl
Farnesyl: proteintransferase inhibitors as agents to inhibit tumor growth.
BioFactors (Oxford, England) 1997;6(3):359-66.
1996: John H Hutchinson; Jacquelynn J Cook; K M Brashear; Michael J Breslin; JD Glass; Robert Gould; W Halczenko; Marie A Holahan; RJ Lynch; Gary R Sitko; Maria T Stranieri; George D Hartman
Non-peptide glycoprotein IIb/IIIa antagonists. 11. Design and in vivo evaluation of 3,4-dihydro-1 (1H)-isoquinolinone-based antagonists and ethyl ester prodrugs.
Journal of medicinal chemistry 1996;39(23):4583-91.
1996: Kenneth S Koblan; Nancy E Kohl; CA Omer; Neville J Anthony; M W Conner; S Jane deSolms; Theresa M Williams; Samuel L Graham; George D Hartman; Allen Oliff; Jackson B Gibbs
Farnesyltransferase inhibitors: a new class of cancer chemotherapeutics.
Biochemical Society transactions 1996;24(3):688-92.
1996: Jacquelynn J Cook; Marie A Holahan; Elizabeth A Lyle; D R Ramjit; Gary R Sitko; Maria T Stranieri; R F Stupienski; Audrey A Wallace; Elizabeth Hand; J R Gehret; T Kothstein; M D Drag; G Y McCormick; J J Perkins; N C Ihle; M E Duggan; George D Hartman; Robert Gould; Joseph J Lynch
Nonpeptide glycoprotein IIb/IIIa inhibitors. 8. Antiplatelet activity and oral antithrombotic efficacy of L-734,217.
The Journal of pharmacology and experimental therapeutics 1996;278(1):62-73.
1996: Theresa M Williams; T M Ciccarone; Suzanne C MacTough; R L Bock; M W Conner; J P Davide; K Hamilton; Kenneth S Koblan; Nancy E Kohl; AM Kral; Scott D Mosser; CA Omer; DL Pompliano; Elaine Rands; Michael D Schaber; D Shah; F R Wilson; Jackson B Gibbs; Samuel L Graham; George D Hartman; Allen Oliff; R L Smith
2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase.
Journal of medicinal chemistry 1996;39(7):1345-8.
1996: Jackson B Gibbs; Nancy E Kohl; Kenneth S Koblan; CA Omer; Laura Sepp-Lorenzino; Neal Rosen; Neville J Anthony; M W Conner; S Jane deSolms; Theresa M Williams; Samuel L Graham; George D Hartman; Allen Oliff
Farnesyltransferase inhibitors and anti-Ras therapy.
Breast cancer research and treatment 1996;38(1):75-83.
1995: M E Duggan; Adel M Naylor-Olsen; J J Perkins; P S Anderson; C T Chang; Jacquelynn J Cook; Robert Gould; N C Ihle; George D Hartman; Joseph J Lynch
Non-peptide fibrinogen receptor antagonists. 7. Design and synthesis of a potent, orally active fibrinogen receptor antagonist.
Journal of medicinal chemistry 1995;38(17):3332-41.
1995: Nancy E Kohl; M W Conner; Jackson B Gibbs; Samuel L Graham; George D Hartman; Allen Oliff
Development of inhibitors of protein farnesylation as potential chemotherapeutic agents.
Journal of cellular biochemistry. Supplement 1995;22():145-50.
1994: Melissa S Egbertson; C T Chang; M E Duggan; Robert Gould; W Halczenko; George D Hartman; W L Laswell; Joseph J Lynch; RJ Lynch; P D Manno
Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp.
Journal of medicinal chemistry 1994;37(16):2537-51.
1994: J S Barrett; Robert Gould; Joan D Ellis; M M Holahan; Maria T Stranieri; Joseph J Lynch; George D Hartman; N Ihle; M Duggan; O A Moreno
Pharmacokinetics and pharmacodynamics of L-703,014, a potent fibrinogen receptor antagonist, after intravenous and oral administration in the dog.
Pharmaceutical research 1994;11(3):426-31.
1992: George D Hartman; Melissa S Egbertson; W Halczenko; W L Laswell; M E Duggan; R L Smith; A M Naylor; P D Manno; RJ Lynch; G Zhang
Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors.
Journal of medicinal chemistry 1992;35(24):4640-2.
1992: George D Hartman; W Halczenko; R L Smith; M F Sugŕue; P J Mallorga; Stuart R Michelson; W C Randall; H Schwam; J M Sondey
4-substituted thiophene- and furan-2-sulfonamides as topical carbonic anhydrase inhibitors.
Journal of medicinal chemistry 1992;35(21):3822-31.
1992: George D Hartman; W Halczenko; M E Duggan; J S Imagire; R L Smith; Steven M Pitzenberger; S L Fitzpatrick; A W Alberts; RG Bostedor; Y S Chao
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 9. The synthesis and biological evaluation of novel simvastatin analogs.
Journal of medicinal chemistry 1992;35(21):3813-21.
1992: George D Hartman; W Halczenko; J D Prugh; R L Smith; M F Sugrue; P Mallorga; Stuart R Michelson; W C Randall; H Schwam; J M Sondey
Thieno[2,3-b]furan-2-sulfonamides as topical carbonic anhydrase inhibitors.
Journal of medicinal chemistry 1992;35(16):3027-33.
1991: M E Duggan; A W Alberts; RG Bostedor; Y S Chao; J I Germershausen; J L Gilfillan; W Halczenko; George D Hartman; V Hunt; J S Imagire
3-Hydroxy-3-methylglutaryl-coenzyme a reductase inhibitors. 7. Modification of the hexahydronaphthalene moiety of simvastatin: 5-oxygenated and 5-oxa derivatives.
Journal of medicinal chemistry 1991;34(8):2489-95.
1991: J D Prugh; George D Hartman; P J Mallorga; Brian McKeever; Stuart R Michelson; M A Murcko; H Schwam; R L Smith; J M Sondey; J P Springer
New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors: 5-substituted thieno[2,3-b]thiophene-2-sulfonamides and 5-substituted thieno[3,2-b]thiophene-2-sulfonamides.
Journal of medicinal chemistry 1991;34(6):1805-18.