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Mark Cushman

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TOP 3
Martin Conda-Sheridan; Daniel E Beck; Lian Chen; Bingjie Hu; Trung X Nguyen; Eun-Jung Park; John M Pezzuto; P V Narasimha Reddy; Richard B Van Breemen; Jerry J White; Mark Cushman
Design, synthesis, and biological evaluation of indenoisoquinoline rexinoids with chemopreventive potential.
Martin Conda-Sheridan; Keli Agama; Lakshman K Bindu; Adel Chergui; Brooklyn T Cobb; Christophe Marchand; Andrew Morrell; Yves Pommier; P V Narasimha Reddy; Amélie Renaud; Andrew G Stephen; Mark Cushman
Synthesis and biological evaluation of indenoisoquinolines that inhibit both tyrosyl-DNA phosphodiesterase I (Tdp1) and topoisomerase I (Top1).
Maris A Cinelli; Keli Agama; Lian Chen; Jian-Hua Liang; Peng-Cheng Lv; Yves Pommier; P V Narasimha Reddy; Richard B Van Breemen; Mark Cushman
Identification, synthesis, and biological evaluation of metabolites of the experimental cancer treatment drugs indotecan (LMP400) and indimitecan (LMP776) and investigation of isomerically hydroxylated indenoisoquinoline analogues as topoisomerase I poisons.

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All Publications

2013: Martin Conda-Sheridan; Daniel E Beck; Lian Chen; Bingjie Hu; Trung X Nguyen; Eun-Jung Park; John M Pezzuto; P V Narasimha Reddy; Richard B Van Breemen; Jerry J White; Mark Cushman
Design, synthesis, and biological evaluation of indenoisoquinoline rexinoids with chemopreventive potential.
Journal of medicinal chemistry 2013;56(6):2581-605.
2013: Martin Conda-Sheridan; Keli Agama; Lakshman K Bindu; Adel Chergui; Brooklyn T Cobb; Christophe Marchand; Andrew Morrell; Yves Pommier; P V Narasimha Reddy; Amélie Renaud; Andrew G Stephen; Mark Cushman
Synthesis and biological evaluation of indenoisoquinolines that inhibit both tyrosyl-DNA phosphodiesterase I (Tdp1) and topoisomerase I (Top1).
Journal of medicinal chemistry 2013;56(1):182-200.
2012: Maris A Cinelli; Keli Agama; Lian Chen; Jian-Hua Liang; Peng-Cheng Lv; Yves Pommier; P V Narasimha Reddy; Richard B Van Breemen; Mark Cushman
Identification, synthesis, and biological evaluation of metabolites of the experimental cancer treatment drugs indotecan (LMP400) and indimitecan (LMP776) and investigation of isomerically hydroxylated indenoisoquinoline analogues as topoisomerase I poisons.
Journal of medicinal chemistry 2012;55(24):10844-62.
2012: Abdelrahman S Mayhoub; Eun-Jung Park; John M Pezzuto; Tamara P Kondratyuk; Laura Marler; Mark Cushman
Optimization of thiazole analogues of resveratrol for induction of NAD(P)H:quinone reductase 1 (QR1).
Bioorganic & medicinal chemistry 2012;20(24):7030-9.
2012: Arindam Talukdar; Yujie Zhao; Adelbert Bacher; Markus Fischer; Boris Illarionov; Wei Lv; Mark Cushman
O-Nucleoside, S-nucleoside, and N-nucleoside probes of lumazine synthase and riboflavin synthase.
The Journal of organic chemistry 2012;77(14):6239-61.
2012: Lian Chen; Martin Conda-Sheridan; Tamara P Kondratyuk; Andrew Morrell; Eun-Jung Park; John M Pezzuto; P V Narasimha Reddy; Richard B Van Breemen; Mark Cushman
Identification, synthesis, and biological evaluation of the metabolites of 3-amino-6-(3'-aminopropyl)-5H-indeno[1,2-c]isoquinoline-5,11-(6H)dione (AM6-36), a promising rexinoid lead compound for the development of cancer chemotherapeutic and chemopreventive agents.
Journal of medicinal chemistry 2012;55(12):5965-81.
2012: Evgeny Kiselev; Yves Pommier; Keli Agama; Nicholas Empey; Mark Cushman
Dibenzo[c,h][1,5]naphthyridinediones as topoisomerase I inhibitors: design, synthesis, and biological evaluation.
The Journal of organic chemistry 2012;77(11):5167-72.
2012: Trung Xuan Nguyen; Yves Pommier; Mark Cushman; Andrew G Stephen; Keli Agama; Alun Bermingam; Alun Bermingham; Adel Chergui; Martin Conda-Sheridan; Robert Fisher; Christophe Marchand; Andrew Morrell; Alena Naumova; Mark Cushman
Synthesis and biological evaluation of the first dual tyrosyl-DNA phosphodiesterase I (Tdp1)-topoisomerase I (Top1) inhibitors.
Journal of medicinal chemistry 2012;55(9):4457-78.
2012: Abdelrahman S Mayhoub; Eun-Jung Park; John M Pezzuto; Tamara P Kondratyuk; Laura Marler; Mark Cushman
Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol.
Bioorganic & medicinal chemistry 2012;20(7):2427-34.
2012: Evgeny Kiselev; Yves Pommier; Keli Agama; Mark Cushman
Azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents: a systematic study of structure-activity relationships.
Journal of medicinal chemistry 2012;55(4):1682-97.
2011: Evgeny Kiselev; Andrew Morrell; Yves Pommier; Keli Agama; Sean DeGuire; Thomas S Dexheimer; Mark Cushman
7-azaindenoisoquinolines as topoisomerase I inhibitors and potential anticancer agents.
Journal of medicinal chemistry 2011;54(17):6106-16.
2011: Katherine E Peterson; Yves Pommier; Thomas S Dexheimer; Akhil Mehta; Andrew Morrell; Keli Agama; Smitha Antony; Maris A Cinelli; Mark Cushman
Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase I inhibitors: investigating the relationships involving stereochemistry, hydrogen bonding, and biological activity.
Journal of medicinal chemistry 2011;54(14):4937-53.
2011: Abdelrahman S Mayhoub; Carolyn Botting; Mansoora Khaliq; Richard J Kuhn; Ze Li; Mark Cushman
An investigation of phenylthiazole antiflaviviral agents.
Bioorganic & medicinal chemistry 2011;19(12):3845-54.
2011: Abdelrahman S Mayhoub; Mansoora Khaliq; Richard J Kuhn; Mark Cushman
Design, synthesis, and biological evaluation of thiazoles targeting flavivirus envelope proteins.
Journal of medicinal chemistry 2011;54(6):1704-14.
2010: Martin Conda-Sheridan; Laura Marler; Eun-Jung Park; Tamara P Kondratyuk; Katherine Jermihov; Andrew D Mesecar; John M Pezzuto; Ratnakar N Asolkar; William Fenical; Mark Cushman
Potential chemopreventive agents based on the structure of the lead compound 2-bromo-1-hydroxyphenazine, isolated from Streptomyces species, strain CNS284.
Journal of medicinal chemistry 2010;53(24):8688-99.
2010: Evgeny Kiselev; Thomas S Dexheimer; Yves Pommier; Mark Cushman
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
Journal of medicinal chemistry 2010;53(24):8716-26.
2010: Ekaterina Morgunova; Boris Illarionov; Sabine Saller; Aleksander Popov; Thota Sambaiah; Adelbert Bacher; Mark Cushman; Markus Fischer; Rudolf Ladenstein
Structural study and thermodynamic characterization of inhibitor binding to lumazine synthase from Bacillus anthracis.
Acta crystallographica. Section D, Biological crystallography 2010;66(Pt 9):1001-11.
2010: Maris A Cinelli; Andrew E Morrell; Thomas S Dexheimer; Keli Agama; Surbhi Agrawal; Yves Pommier; Mark Cushman
The structure-activity relationships of A-ring-substituted aromathecin topoisomerase I inhibitors strongly support a camptothecin-like binding mode.
Bioorganic & medicinal chemistry 2010;18(15):5535-52.
2010: Bin Sun; Juma Hoshino; Katie Jermihov; Laura Marler; John M Pezzuto; Andrew D Mesecar; Mark Cushman
Design, synthesis, and biological evaluation of resveratrol analogues as aromatase and quinone reductase 2 inhibitors for chemoprevention of cancer.
Bioorganic & medicinal chemistry 2010;18(14):5352-66.
2010: Juma Hoshino; Eun-Jung Park; Tamara P Kondratyuk; Laura Marler; John M Pezzuto; Richard B Van Breemen; Shunyan Mo; Yongchao Li; Mark Cushman
Selective synthesis and biological evaluation of sulfate-conjugated resveratrol metabolites.
Journal of medicinal chemistry 2010;53(13):5033-43.
2010: P V Narasimha Reddy; Biplab Banerjee; Mark Cushman
Efficient total synthesis of ammosamide B.
Organic letters 2010;12(13):3112-4.
2010: Abdelrahman S Mayhoub; Arindam Talukdar; Mark Cushman
An oxidation of benzyl methyl ethers with nbs that selectively affords either aromatic aldehydes or aromatic methyl esters.
The Journal of organic chemistry 2010;75(10):3507-10.
2010: Arindam Talukdar; Ekaterina Morgunova; Jianxin Duan; Winfried Meining; Nicolas Foloppe; Lennart Nilsson; Adelbert Bacher; Boris Illarionov; Markus Fischer; Rudolf Ladenstein; Mark Cushman
Virtual screening, selection and development of a benzindolone structural scaffold for inhibition of lumazine synthase.
Bioorganic & medicinal chemistry 2010;18(10):3518-34.
2010: Yunlong Song; Zhiyu Shao; Thomas S Dexheimer; Evan S Scher; Yves Pommier; Mark Cushman
Structure-based design, synthesis, and biological studies of new anticancer norindenoisoquinoline topoisomerase I inhibitors.
Journal of medicinal chemistry 2010;53(5):1979-89.
2009: Matthew D Cullen; William C Ho; Joseph D Bauman; Kalyan Das; Eddy Arnold; Tracy L Hartman; Karen M Watson; Robert W Buckheit; Christophe Pannecouque; Erik De Clercq; Mark Cushman
Crystallographic study of a novel subnanomolar inhibitor provides insight on the binding interactions of alkenyldiarylmethanes with human immunodeficiency virus-1 reverse transcriptase.
Journal of medicinal chemistry 2009;52(20):6467-73.
2009: Maris A Cinelli; Brenda Cordero; Thomas S Dexheimer; Yves Pommier; Mark Cushman
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
Bioorganic & medicinal chemistry 2009;17(20):7145-55.
2009: Arindam Talukdar; Meghan Breen; Adelbert Bacher; Boris Illarionov; Markus Fischer; Gunda I Georg; Qi-Zhuang Ye; Mark Cushman
Discovery and development of a small molecule library with lumazine synthase inhibitory activity.
The Journal of organic chemistry 2009;74(15):5123-34.
2009: Yujie Zhao; Adelbert Bacher; Boris Illarionov; Markus Fischer; Gunda I Georg; Qi-Zhuang Ye; Phillip E Fanwick; Scott Franzblau; Baojie Wan; Mark Cushman
Discovery and development of the covalent hydrates of trifluoromethylated pyrazoles as riboflavin synthase inhibitors with antibiotic activity against Mycobacterium tuberculosis.
The Journal of organic chemistry 2009;74(15):5297-303.
2009: Yves Pommier; Mark Cushman
The indenoisoquinoline noncamptothecin topoisomerase I inhibitors: update and perspectives.
Molecular cancer therapeutics 2009;8(5):1008-14.
2009: Arup Maiti; P V Narasimha Reddy; Megan Sturdy; Laura Marler; Scott D Pegan; Andrew D Mesecar; John M Pezzuto; Mark Cushman
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.
Journal of medicinal chemistry 2009;52(7):1873-84.
2009: Bo-Liang Deng; Yujie Zhao; Tracy L Hartman; Karen Watson; Robert W Buckheit; Christophe Pannecouque; Erik De Clercq; Mark Cushman
Synthesis of alkenyldiarylmethanes (ADAMs) containing benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
European journal of medicinal chemistry 2009;44(3):1210-4.
2008: Tsyr-Yan Yu; Robert D O'Connor; Astrid Sivertsen; Colby Chiauzzi; Barbara Poliks; Markus Fischer; Adelbert Bacher; Ilka Haase; Mark Cushman; Jacob Schaefer
(15)N{(31)P} REDOR NMR studies of the binding of phosphonate reaction intermediate analogues to Saccharomyces cerevisiae lumazine synthase.
Biochemistry 2008;47(52):13942-51.
2008: Muriel Cuendet; Carol P Oteham; Arup Maiti; Bruce A Craig; Mark Cushman; Richard C Moon; John M Pezzuto
Zapotin prevents mouse skin tumorigenesis during the stages of initiation and promotion.
Anticancer research 2008;28(6A):3705-9.
2008: Zhenglai Fang; Yunlong Song; Taradas Sarkar; Ernest Hamel; William E Fogler; Gregory E Agoston; Phillip E Fanwick; Mark Cushman
Stereoselective synthesis of 3,3-diarylacrylonitriles as tubulin polymerization inhibitors.
The Journal of organic chemistry 2008;73(11):4241-4.
2008: Yanlei Zhang; Boris Illarionov; Ekaterina Morgunova; Guangyi Jin; Adelbert Bacher; Markus Fischer; Rudolf Ladenstein; Mark Cushman
A new series of N-[2,4-dioxo-6-d-ribitylamino-1,2,3,4-tetrahydropyrimidin-5-yl]oxalamic acid derivatives as inhibitors of lumazine synthase and riboflavin synthase: design, synthesis, biochemical evaluation, crystallography, and mechanistic implications.
The Journal of organic chemistry 2008;73(7):2715-24.
2008: Matthew Cullen; Deborah Miles; Arlene P Rothwell; Connie C Bonham; Karl V Wood; Mark Cushman
Hydrolysis of thioesters in an ion trap.
Rapid communications in mass spectrometry : RCM 2008;22(8):1094-8.
2008: Matthew D Cullen; York-Fong Cheung; Miles D Houslay; Tracy L Hartman; Karen M Watson; Robert W Buckheit; Christophe Pannecouque; Erik De Clercq; Mark Cushman
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(4):1530-3.
2008: Matthew D Cullen; Taradas Sarkar; Ernest Hamel; Tracy L Hartman; Karen M Watson; Robert W Buckheit; Christophe Pannecouque; Erik De Clercq; Mark Cushman
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
Bioorganic & medicinal chemistry letters 2008;18(2):469-73.
2007: Allison B Edsall; Gregory E Agoston; Anthony M Treston; Stacy M Plum; Robert H McClanahan; Tian-Sheng Lu; Wei Song; Mark Cushman
Synthesis and in vivo antitumor evaluation of 2-methoxyestradiol 3-phosphate, 17-phosphate, and 3,17-diphosphate.
Journal of medicinal chemistry 2007;50(26):6700-5.
2007: Smitha Antony; Keli Agama; Ze-Hong Miao; Kazutaka Takagi; Mollie H Wright; Ana I Robles; Lyuba Varticovski; Muthukaman Nagarajan; Andrew Morrell; Mark Cushman; Yves Pommier
Novel indenoisoquinolines NSC 725776 and NSC 724998 produce persistent topoisomerase I cleavage complexes and overcome multidrug resistance.
Cancer research 2007;67(21):10397-405.
2007: Matthew D Cullen; Bo-Liang Deng; Tracy L Hartman; Karen M Watson; Robert W Buckheit; Christophe Pannecouque; Erik De Clercq; Mark Cushman
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
Journal of medicinal chemistry 2007;50(20):4854-67.
2007: Yanlei Zhang; Guangyi Jin; Boris Illarionov; Adelbert Bacher; Markus Fischer; Mark Cushman
A new series of 3-alkyl phosphate derivatives of 4,5,6,7-tetrahydro-1-D-ribityl-1H-pyrazolo[3,4-d]pyrimidinedione as inhibitors of lumazine synthase: design, synthesis, and evaluation.
The Journal of organic chemistry 2007;72(19):7176-84.
2007: Arindam Talukdar; Boris Illarionov; Adelbert Bacher; Markus Fischer; Mark Cushman
Synthesis and enzyme inhibitory activity of the s-nucleoside analogue of the ribitylaminopyrimidine substrate of lumazine synthase and product of riboflavin synthase.
The Journal of organic chemistry 2007;72(19):7167-75.
2007: Andrew Morrell; Michael Placzek; Seth Parmley; Smitha Antony; Thomas S Dexheimer; Yves Pommier; Mark Cushman
Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.
Journal of medicinal chemistry 2007;50(18):4419-30.
2007: Andrew Morrell; Michael Placzek; Seth Parmley; Brian Grella; Smitha Antony; Yves Pommier; Mark Cushman
Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
Journal of medicinal chemistry 2007;50(18):4388-404.
2007: Takeshi Sakamoto; Matthew D Cullen; Tracy L Hartman; Karen M Watson; Robert W Buckheit; Christophe Pannecouque; Erik De Clercq; Mark Cushman
Synthesis and anti-HIV activity of new metabolically stable alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors incorporating N-methoxy imidoyl halide and 1,2,4-oxadiazole systems.
Journal of medicinal chemistry 2007;50(14):3314-21.
2007: Arup Maiti; Muriel Cuendet; Vicki L Croy; Denise C Endringer; John M Pezzuto; Mark Cushman
Synthesis and biological evaluation of (+/-)-abyssinone II and its analogues as aromatase inhibitors for chemoprevention of breast cancer.
Journal of medicinal chemistry 2007;50(12):2799-806.
2007: Ekaterina Morgunova; Sabine Saller; Ilka Haase; Mark Cushman; Adelbert Bacher; Markus Fischer; Rudolf Ladenstein
Lumazine synthase from Candida albicans as an anti-fungal target enzyme: structural and biochemical basis for drug design.
The Journal of biological chemistry 2007;282(23):17231-41.
2007: Johannes Kaiser; Boris Illarionov; Felix Rohdich; Wolfgang Eisenreich; Sabine Saller; Jan Van den Brulle; Mark Cushman; Adelbert Bacher; Markus Fischer
A high-throughput screening platform for inhibitors of the riboflavin biosynthesis pathway.
Analytical biochemistry 2007;365(1):52-61.
2007: Andrew Morrell; Michael Placzek; Jamin D Steffen; Smitha Antony; Keli Agama; Yves Pommier; Mark Cushman
Investigation of the lactam side chain length necessary for optimal indenoisoquinoline topoisomerase I inhibition and cytotoxicity in human cancer cell cultures.
Journal of medicinal chemistry 2007;50(9):2040-8.
2007: Yanlei Zhang; Boris Illarionov; Adelbert Bacher; Markus Fischer; Gunda I Georg; Qi-Zhuang Ye; David VanderVelde; Phillip E Fanwick; Yunlong Song; Mark Cushman
A novel lumazine synthase inhibitor derived from oxidation of 1,3,6,8-tetrahydroxy-2,7-naphthyridine to a tetraazaperylenehexaone derivative.
The Journal of organic chemistry 2007;72(8):2769-76.
2007: Ha Young Kim; Richard J Kuhn; Chinmay G Patkar; Ranjit Warrier; Mark Cushman
Synthesis of dioxane-based antiviral agents and evaluation of their biological activities as inhibitors of Sindbis virus replication.
Bioorganic & medicinal chemistry 2007;15(7):2667-79.
2007: Chan Yong Lee; Boris Illarionov; Young-Eun Woo; Kristina Kemter; Ryu-Ryun Kim; Sabine Eberhardt; Mark Cushman; Wolfgang Eisenreich; Markus Fischer; Adelbert Bacher
Ligand binding properties of the N-terminal domain of riboflavin synthase from Escherichia coli.
Journal of biochemistry and molecular biology 2007;40(2):239-46.
2007: Arup Maiti; Muriel Cuendet; Tamara Kondratyuk; Vicki L Croy; John M Pezzuto; Mark Cushman
Synthesis and cancer chemopreventive activity of zapotin, a natural product from Casimiroa edulis.
Journal of medicinal chemistry 2007;50(2):350-5.
2006: Andrew Morrell; Smitha Antony; Glenda Kohlhagen; Yves Pommier; Mark Cushman
A systematic study of nitrated indenoisoquinolines reveals a potent topoisomerase I inhibitor.
Journal of medicinal chemistry 2006;49(26):7740-53.
2006: Muthukaman Nagarajan; Andrew Morrell; Alexandra Ioanoviciu; Smitha Antony; Glenda Kohlhagen; Keli Agama; Melinda G Hollingshead; Yves Pommier; Mark Cushman
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.
Journal of medicinal chemistry 2006;49(21):6283-9.
2006: Ekaterina Morgunova; Boris Illarionov; Thota Sambaiah; Ilka Haase; Adelbert Bacher; Mark Cushman; Markus Fischer; Rudolf Ladenstein
Structural and thermodynamic insights into the binding mode of five novel inhibitors of lumazine synthase from Mycobacterium tuberculosis.
The FEBS journal 2006;273(20):4790-804.
2006: Smitha Antony; Keli Agama; Ze-Hong Miao; Melinda G Hollingshead; Susan Holbeck; Mollie H Wright; Lyuba Varticovski; Muthukaman Nagarajan; Andrew Morrell; Mark Cushman; Yves Pommier
Bisindenoisoquinoline bis-1,3-{(5,6-dihydro-5,11-diketo-11H-indeno[1,2-c]isoquinoline)-6-propylamino}propane bis(trifluoroacetate) (NSC 727357), a DNA intercalator and topoisomerase inhibitor with antitumor activity.
Molecular pharmacology 2006;70(3):1109-20.
2006: Bo-Liang Deng; Tracy L Hartman; Robert W Buckheit; Christophe Pannecouque; Erik De Clercq; Mark Cushman
Replacement of the metabolically labile methyl esters in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors with isoxazolone, isoxazole, oxazolone, or cyano substituents.
Journal of medicinal chemistry 2006;49(17):5316-23.
2006: Muthukaman Nagarajan; Andrew Morrell; Smitha Antony; Glenda Kohlhagen; Keli Agama; Yves Pommier; Patricia A Ragazzon; Nichola C Garbett; Jonathan B Chaires; Melinda G Hollingshead; Mark Cushman
Synthesis and biological evaluation of bisindenoisoquinolines as topoisomerase I inhibitors.
Journal of medicinal chemistry 2006;49(17):5129-40.
2006: Andrew Morrell; Muthusamy Jayaraman; Muthukaman Nagarajan; Brian M Fox; Marintha Rae Meckley; Alexandra Ioanoviciu; Yves Pommier; Smitha Antony; Melinda G Hollingshead; Mark Cushman
Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay.
Bioorganic & medicinal chemistry letters 2006;16(16):4395-9.
2006: Nwanne O Anadu; V Jo Davisson; Mark Cushman
Synthesis and anticancer activity of brefeldin A ester derivatives.
Journal of medicinal chemistry 2006;49(13):3897-905.
2006: Andrew Morrell; Smitha Antony; Glenda Kohlhagen; Yves Pommier; Mark Cushman
Synthesis of benz[d]indeno[1,2-b]pyran-5,11-diones: versatile intermediates for the design and synthesis of topoisomerase I inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(7):1846-9.
2006: Bo-Liang Deng; Matthew D Cullen; Zhigang Zhou; Tracy L Hartman; Robert W Buckheit; Christophe Pannecouque; Erik De Clercq; Phillip E Fanwick; Mark Cushman
Synthesis and anti-HIV activity of new alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors (NNRTIs) incorporating benzoxazolone and benzisoxazole rings.
Bioorganic & medicinal chemistry 2006;14(7):2366-74.
2006: Ha Young Kim; Arindam Talukdar; Mark Cushman
Regioselective synthesis of N-beta-hydroxyethylaziridines by the ring-opening reaction of epoxides with aziridine generated in situ.
Organic letters 2006;8(6):1085-7.
2006: Xiangshu Xiao; Smitha Antony; Yves Pommier; Mark Cushman
Total synthesis and biological evaluation of 22-hydroxyacuminatine.
Journal of medicinal chemistry 2006;49(4):1408-12.
2006: Christophe Marchand; Smitha Antony; Kurt W Kohn; Mark Cushman; Alexandra Ioanoviciu; Bart L Staker; Alex B Burgin; Lance Stewart; Yves Pommier
A novel norindenoisoquinoline structure reveals a common interfacial inhibitor paradigm for ternary trapping of the topoisomerase I-DNA covalent complex.
Molecular cancer therapeutics 2006;5(2):287-95.
2006: Arne Ramsperger; Martin Augustin; Anne-Kathrin Schott; Stefan Gerhardt; Tobias Krojer; Wolfgang Eisenreich; Boris Illarionov; Mark Cushman; Adelbert Bacher; Robert Huber; Markus Fischer
Crystal structure of an archaeal pentameric riboflavin synthase in complex with a substrate analog inhibitor: stereochemical implications.
The Journal of biological chemistry 2006;281(2):1224-32.
2005: Xiangshu Xiao; Mark Cushman
Effect of E-ring modifications in camptothecin on topoisomerase I inhibition: a quantum mechanics treatment.
The Journal of organic chemistry 2005;70(23):9584-7.
2005: Mark Cushman; Guangyi Jin; Thota Sambaiah; Boris Illarionov; Markus Fischer; Rudolf Ladenstein; Adelbert Bacher
Design, synthesis, and biochemical evaluation of 1,5,6,7-tetrahydro-6,7-dioxo-9-D-ribitylaminolumazines bearing alkyl phosphate substituents as inhibitors of lumazine synthase and riboflavin synthase.
The Journal of organic chemistry 2005;70(20):8162-70.
2005: Bo-Liang Deng; Tracy L Hartman; Robert W Buckheit; Christophe Pannecouque; Erik De Clercq; Phillip E Fanwick; Mark Cushman
Synthesis, anti-HIV activity, and metabolic stability of new alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry 2005;48(19):6140-55.
2005: Xiangshu Xiao; Mark Cushman
A Facile method to transform trans-4-carboxy-3,4-dihydro-3-phenyl- 1(2H)-isoquinolones to indeno[1,2-c]isoquinolines.
The Journal of organic chemistry 2005;70(16):6496-8.
2005: Alexandra Ioanoviciu; Smitha Antony; Yves Pommier; Bart L Staker; Lance Stewart; Mark Cushman
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis.
Journal of medicinal chemistry 2005;48(15):4803-14.
2005: Xiangshu Xiao; Mark Cushman
An ab initio quantum mechanics calculation that correlates with ligand orientation and DNA cleavage site selectivity in camptothecin-DNA-topoisomerase I ternary cleavage complexes.
Journal of the American Chemical Society 2005;127(28):9960-1.
2005: Ha Young Kim; Chinmay G Patkar; Ranjit Warrier; Richard Kuhn; Mark Cushman
Design, synthesis, and evaluation of dioxane-based antiviral agents targeted against the Sindbis virus capsid protein.
Bioorganic & medicinal chemistry letters 2005;15(13):3207-11.
2005: Xiangshu Xiao; Ze-Hong Miao; Smitha Antony; Yves Pommier; Mark Cushman
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
Bioorganic & medicinal chemistry letters 2005;15(11):2795-8.
2005: Xiangshu Xiao; Smitha Antony; Yves Pommier; Mark Cushman
On the binding of indeno[1,2-c]isoquinolines in the DNA-topoisomerase I cleavage complex.
Journal of medicinal chemistry 2005;48(9):3231-8.
2005: Bart L Staker; Michael D Feese; Mark Cushman; Yves Pommier; David Zembower; Lance Stewart; Alex B Burgin
Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex.
Journal of medicinal chemistry 2005;48(7):2336-45.
2005: Ekaterina Morgunova; Winfried Meining; Boris Illarionov; Ilka Haase; Guangyi Jin; Adelbert Bacher; Mark Cushman; Markus Fischer; Rudolf Ladenstein
Crystal structure of lumazine synthase from Mycobacterium tuberculosis as a target for rational drug design: binding mode of a new class of purinetrione inhibitors.
Biochemistry 2005;44(8):2746-58.
2005: Jinhua Chen; Boris Illarionov; Adelbert Bacher; Markus Fischer; Ilka Haase; Gunda I Georg; Qi-Zhuang Ye; Zeqiang Ma; Mark Cushman
A high-throughput screen utilizing the fluorescence of riboflavin for identification of lumazine synthase inhibitors.
Analytical biochemistry 2005;338(1):124-30.
2005: Smitha Antony; Glenda Kohlhagen; Keli Agama; Muthusamy Jayaraman; Shousong Cao; Farukh A Durrani; Youcef M Rustum; Mark Cushman; Yves Pommier
Cellular topoisomerase I inhibition and antiproliferative activity by MJ-III-65 (NSC 706744), an indenoisoquinoline topoisomerase I poison.
Molecular pharmacology 2005;67(2):523-30.
2004: Muthukaman Nagarajan; Andrew Morrell; Brian C Fort; Marintha Rae Meckley; Smitha Antony; Glenda Kohlhagen; Yves Pommier; Mark Cushman
Synthesis and anticancer activity of simplified indenoisoquinoline topoisomerase I inhibitors lacking substituents on the aromatic rings.
Journal of medicinal chemistry 2004;47(23):5651-61.
2004: Xiangshu Xiao; Smitha Antony; Glenda Kohlhagen; Yves Pommier; Mark Cushman
Novel autoxidative cleavage reaction of 9-fluoredenes discovered during synthesis of a potential DNA-threading indenoisoquinoline.
The Journal of organic chemistry 2004;69(22):7495-501.
2004: Jinhua Chen; Thota Sambaiah; Boris Illarionov; Markus Fischer; Adelbert Bacher; Mark Cushman
Design, synthesis, and evaluation of acyclic C-nucleoside and N-methylated derivatives of the ribitylaminopyrimidine substrate of lumazine synthase as potential enzyme inhibitors and mechanistic probes.
The Journal of organic chemistry 2004;69(21):6996-7003.
2004: Allison B Edsall; Arasambattu K Mohanakrishnan; Donglai Yang; Phillip E Fanwick; Ernest Hamel; Arthur D Hanson; Gregory E Agoston; Mark Cushman
Effects of altering the electronics of 2-methoxyestradiol on cell proliferation, on cytotoxicity in human cancer cell cultures, and on tubulin polymerization.
Journal of medicinal chemistry 2004;47(21):5126-39.
2004: Xiangshu Xiao; Smitha Antony; Glenda Kohlhagen; Yves Pommier; Mark Cushman
Design, synthesis, and biological evaluation of cytotoxic 11-aminoalkenylindenoisoquinoline and 11-diaminoalkenylindenoisoquinoline topoisomerase I inhibitors.
Bioorganic & medicinal chemistry 2004;12(19):5147-60.
2004: Michael Koch; Constanze Breithaupt; StefanIlka GerhardtHaase; Stefan Weber; Mark Cushman; Robert Huber; Adelbert Bacher; Markus Fischer
Structural basis of charge transfer complex formation by riboflavin bound to 6,7-dimethyl-8-ribityllumazine synthase.
European journal of biochemistry / FEBS 2004;271(15):3208-14.
2004: Andrew Morrell; Smitha Antony; Glenda Kohlhagen; Yves Pommier; Mark Cushman
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(14):3659-63.
2004: Maximilian Silvestri; Muthukaman Nagarajan; Erik De Clercq; Christophe Pannecouque; Mark Cushman
Design, synthesis, anti-HIV activities, and metabolic stabilities of alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry 2004;47(12):3149-62.
2004: Mark Cushman; Thota Sambaiah; Guangyi Jin; Boris Illarionov; Markus Fischer; Adelbert Bacher
Design, synthesis, and evaluation of 9-D-ribitylamino-1,3,7,9-tetrahydro-2,6,8-purinetriones bearing alkyl phosphate and alpha,alpha-difluorophosphonate substituents as inhibitors of tiboflavin synthase and lumazine synthase.
The Journal of organic chemistry 2004;69(3):601-12.
2003: Markus Fischer; Anne-Kathrin Schott; Kristina Kemter; Richard Feicht; Gerald Richter; Boris Illarionov; Wolfgang Eisenreich; Stefan Gerhardt; Mark Cushman; Stefan Steinbacher; Robert Huber; Adelbert Bacher
Riboflavin synthase of Schizosaccharomyces pombe. Protein dynamics revealed by 19F NMR protein perturbation experiments.
BMC biochemistry 2003;4():18.
2003: Muthukaman Nagarajan; Xiangshu Xiao; Smitha Antony; Glenda Kohlhagen; Yves Pommier; Mark Cushman
Design, synthesis, and biological evaluation of indenoisoquinoline topoisomerase I inhibitors featuring polyamine side chains on the lactam nitrogen.
Journal of medicinal chemistry 2003;46(26):5712-24.
2003: Smitha Antony; Muthusamy Jayaraman; Gary S Laco; Glenda Kohlhagen; Kurt W Kohn; Mark Cushman; Yves Pommier
Differential induction of topoisomerase I-DNA cleavage complexes by the indenoisoquinoline MJ-III-65 (NSC 706744) and camptothecin: base sequence analysis and activity against camptothecin-resistant topoisomerases I.
Cancer research 2003;63(21):7428-35.
2003: Brian M Fox; Xiangshu Xiao; Smitha Antony; Glenda Kohlhagen; Yves Pommier; Bart L Staker; Lance Stewart; Mark Cushman
Design, synthesis, and biological evaluation of cytotoxic 11-alkenylindenoisoquinoline topoisomerase I inhibitors and indenoisoquinoline-camptothecin hybrids.
Journal of medicinal chemistry 2003;46(15):3275-82.
2003: Fanrong Mu; Ernest Hamel; Debbie J Lee; Donald E Pryor; Mark Cushman
Synthesis, anticancer activity, and inhibition of tubulin polymerization by conformationally restricted analogues of lavendustin A.
Journal of medicinal chemistry 2003;46(9):1670-82.
2003: Xiaofeng Zhang; Winfried Meining; Mark Cushman; Ilka Haase; Markus Fischer; Adelbert Bacher; Rudolf Ladenstein
A structure-based model of the reaction catalyzed by lumazine synthase from Aquifex aeolicus.
Journal of molecular biology 2003;328(1):167-82.
2003: Markus Fischer; Ilka Haase; Klaus Kis; Winfried Meining; Rudolf Ladenstein; Mark Cushman; Nicholas Schramek; Robert Huber; Adelbert Bacher
Enzyme catalysis via control of activation entropy: site-directed mutagenesis of 6,7-dimethyl-8-ribityllumazine synthase.
Journal of molecular biology 2003;326(3):783-93.
2003: Maximilian Silvestri; Deborah Miles; Arlene P Rothwell; Karl V Wood; Mark Cushman
The 'apparent' hydrolysis of alkyl esters during electrospray ionization.
Rapid communications in mass spectrometry : RCM 2003;17(15):1703-8.
2002: Fanrong Mu; Debbie J Lee; Donald E Pryor; Ernest Hamel; Mark Cushman
Synthesis and investigation of conformationally restricted analogues of lavendustin A as cytotoxic inhibitors of tubulin polymerization.
Journal of medicinal chemistry 2002;45(21):4774-85.
2002: Mark Cushman; Arasambattu K Mohanakrishnan; Melinda G Hollingshead; Ernest Hamel
The effect of exchanging various substituents at the 2-position of 2-methoxyestradiol on cytotoxicity in human cancer cell cultures and inhibition of tubulin polymerization.
Journal of medicinal chemistry 2002;45(21):4748-54.
2002: Mark Cushman; Donglai Yang; Jeffrey T Mihalic; Jinhua Chen; Stefan Gerhardt; Robert Huber; Markus Fischer; Klaus Kis; Adelbert Bacher
Incorporation of an amide into 5-phosphonoalkyl-6-D-ribitylaminopyrimidinedione lumazine synthase inhibitors results in an unexpected reversal of selectivity for riboflavin synthase vs lumazine synthase.
The Journal of organic chemistry 2002;67(20):6871-7.
2002: Stefan Gerhardt; Anne-Kathrin Schott; Norman Kairies; Mark Cushman; Boris Illarionov; Wolfgang Eisenreich; Adelbert Bacher; Robert Huber; Stefan Steinbacher; Markus Fischer
Studies on the reaction mechanism of riboflavin synthase: X-ray crystal structure of a complex with 6-carboxyethyl-7-oxo-8-ribityllumazine.
Structure (London, England : 1993) 2002;10(10):1371-81.
2002: Mark Cushman; Donglai Yang; Stefan Gerhardt; Robert Huber; Markus Fischer; Klaus Kis; Adelbert Bacher
Design, synthesis, and evaluation of 6-carboxyalkyl and 6-phosphonoxyalkyl derivatives of 7-oxo-8-ribitylaminolumazines as inhibitors of riboflavin synthase and lumazine synthase.
The Journal of organic chemistry 2002;67(16):5807-16.
2002: Guozhang Xu; Arunachalam Kannan; Tracy L Hartman; Heather Wargo; Karen Watson; Jim A Turpin; Robert W Buckheit; Allison A Johnson; Yves Pommier; Mark Cushman
Synthesis of substituted diarylmethylenepiperidines (DAMPs), a novel class of anti-HIV agents.
Bioorganic & medicinal chemistry 2002;10(8):2807-16.
2002: Stefan Gerhardt; Ilka Haase; Stefan Steinbacher; Jens Thomas Kaiser; Mark Cushman; Adelbert Bacher; Robert Huber; Markus Fischer
The structural basis of riboflavin binding to Schizosaccharomyces pombe 6,7-dimethyl-8-ribityllumazine synthase.
Journal of molecular biology 2002;318(5):1317-29.
2002: Anil K Mehta; Daniel R Studelska; Markus Fischer; Andreas Giessauf; Kristina Kemter; Adelbert Bacher; Mark Cushman; Jacob Schaefer
Investigation of the binding of epimer A of the covalent hydrate of 6,7-bis(trifluoromethyl)-8-D-ribityllumazine to a recombinant F22W Bacillus subtilis lumazine synthase mutant by (15)N[(19)F] REDOR NMR.
The Journal of organic chemistry 2002;67(7):2087-92.
2002: Guozhang Xu; Tracy L Hartman; Heather Wargo; Jim A Turpin; Robert W Buckheit; Mark Cushman
Synthesis of alkenyldiarylmethane (ADAM) non-nucleoside HIV-1 reverse transcriptase inhibitors with non-identical aromatic rings.
Bioorganic & medicinal chemistry 2002;10(2):283-90.
2002: Muthusamy Jayaraman; Brian M Fox; Melinda G Hollingshead; Glenda Kohlhagen; Yves Pommier; Mark Cushman
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
Journal of medicinal chemistry 2002;45(1):242-9.
2001: Mark Cushman; Donglai Yang; Klaus Kis; Adelbert Bacher
Design, synthesis, and evaluation of 9-D-ribityl-1,3,7-trihydro-2,6,8-purinetrione, a potent inhibitor of riboflavin synthase and lumazine synthase.
The Journal of organic chemistry 2001;66(25):8320-7.
2001: Guozhang Xu; M Micklatcher; Maximilian Silvestri; Tracy L Hartman; J Burrier; MC Osterling; Heather Wargo; Jim A Turpin; Robert W Buckheit; Mark Cushman
The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry 2001;44(24):4092-113.
2001: Brian M Fox; JA Vroman; Phillip E Fanwick; Mark Cushman
Preparation and evaluation of sulfide derivatives of the antibiotic brefeldin a as potential prodrug candidates with enhanced aqueous solubilities.
Journal of medicinal chemistry 2001;44(23):3915-24.
2001: A Casimiro-Garcia; Erik De Clercq; Christophe Pannecouque; M Witvrouw; TL Loftus; Jim A Turpin; Robert W Buckheit; Phillip E Fanwick; Mark Cushman
Synthesis and anti-HIV activity of cosalane analogues incorporating two dichlorodisalicylmethane pharmacophore fragments.
Bioorganic & medicinal chemistry 2001;9(11):2827-41.
2001: Guozhang Xu; TL Loftus; Heather Wargo; Jim A Turpin; Robert W Buckheit; Mark Cushman
Solid-phase synthesis of the alkenyldiarylmethane (ADAM) series of non-nucleoside HIV-1 reverse transcriptase inhibitors.
The Journal of organic chemistry 2001;66(18):5958-64.
2001: Sabine Eberhardt; N Zingler; Kristina Kemter; Gerald Richter; Mark Cushman; Adelbert Bacher
Domain structure of riboflavin synthase.
European journal of biochemistry / FEBS 2001;268(15):4315-23.
2001: Thota Sambaiah; Phillip E Fanwick; Mark Cushman
Investigation of an unexpected addition reaction that occurs when 2,3:4,5-di-O-isopropylidene-D-ribose diethyl dithioacetal is treated with mercuric oxide and mercuric chloride.
The Journal of organic chemistry 2001;66(12):4405-8.
2001: Boris Illarionov; Kristina Kemter; Sabine Eberhardt; Gerald Richter; Mark Cushman; Adelbert Bacher
Riboflavin synthase of Escherichia coli. Effect of single amino acid substitutions on reaction rate and ligand binding properties.
The Journal of biological chemistry 2001;276(15):11524-30.
2001: K C Santhosh; G C Paul; Erik De Clercq; Christophe Pannecouque; M Witvrouw; TL Loftus; Jim A Turpin; Robert W Buckheit; Mark Cushman
Correlation of anti-HIV activity with anion spacing in a series of cosalane analogues with extended polycarboxylate pharmacophores.
Journal of medicinal chemistry 2001;44(5):703-14.
2001: Fanrong Mu; Stephanie L Coffing; David J Riese; Robert L Geahlen; P Verdier-Pinard; T E Hamel; J Johnson; Mark Cushman
Design, synthesis, and biological evaluation of a series of lavendustin A analogues that inhibit EGFR and Syk tyrosine kinases, as well as tubulin polymerization.
Journal of medicinal chemistry 2001;44(3):441-52.
2001: O M Zack Howard; Hui Fang Dong; Joost J Oppenheim; S Insaf; K C Santhosh; G Paul; Mark Cushman
Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds.
Bioorganic & medicinal chemistry letters 2001;11(1):59-62.
2000: K C Santhosh; Erik De Clercq; Christophe Pannecouque; M Witvrouw; TL Loftus; Jim A Turpin; Robert W Buckheit; Mark Cushman
Anti-HIV activity of a series of cosalane amino acid conjugates.
Bioorganic & medicinal chemistry letters 2000;10(22):2505-8.
2000: Mark Cushman; Muthusamy Jayaraman; JA Vroman; A K Fukunaga; Brian M Fox; Glenda Kohlhagen; D Strumberg; Yves Pommier
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
Journal of medicinal chemistry 2000;43(20):3688-98.
2000: G C Paul; Erik De Clercq; Christophe Pannecouque; M Witvrouw; TL Loftus; Jim A Turpin; Robert W Buckheit; Mark Cushman
Identification of optimal anion spacing for anti-HIV activity in a series of cosalane tetracarboxylates.
Bioorganic & medicinal chemistry letters 2000;10(18):2149-52.
2000: Z Wang; Donglai Yang; Arasambattu K Mohanakrishnan; Phillip E Fanwick; P Nampoothiri; Ernest Hamel; Mark Cushman
Synthesis of B-ring homologated estradiol analogues that modulate tubulin polymerization and microtubule stability.
Journal of medicinal chemistry 2000;43(12):2419-29.
2000: Winfried Meining; S Mörtl; Markus Fischer; Mark Cushman; Adelbert Bacher; Rudolf Ladenstein
The atomic structure of pentameric lumazine synthase from Saccharomyces cerevisiae at 1.85 A resolution reveals the binding mode of a phosphonate intermediate analogue.
Journal of molecular biology 2000;299(1):181-97.
2000: A Casimiro-Garcia; Erik De Clercq; Christophe Pannecouque; M Witvrouw; TL Stup; Jim A Turpin; Robert W Buckheit; Mark Cushman
Synthesis and anti-HIV activity of cosalane analogues incorporating nitrogen in the linker chain.
Bioorganic & medicinal chemistry 2000;8(1):191-200.
1999: A Casimiro-Garcia; M Micklatcher; Jim A Turpin; TL Stup; K Watson; Robert W Buckheit; Mark Cushman
Novel modifications in the alkenyldiarylmethane (ADAM) series of non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry 1999;42(23):4861-74.
1999: Mark Cushman; S Insaf; G Paul; JA Ruell; E De Clercq; D Schols; C Pannecouque; M Witvrouw; CA Schaeffer; Jim A Turpin; K Williamson; William G Rice
Extension of the polyanionic cosalane pharmacophore as a strategy for increasing anti-HIV potency.
Journal of medicinal chemistry 1999;42(10):1767-77.
1999: D Strumberg; Yves Pommier; KD Paull; Muthusamy Jayaraman; P Nagafuji; Mark Cushman
Synthesis of cytotoxic indenoisoquinoline topoisomerase I poisons.
Journal of medicinal chemistry 1999;42(3):446-57.
1999: Mark Cushman; J T Mihalic; Klaus Kis; Adelbert Bacher
Design and synthesis of 6-(6-D-ribitylamino-2,4-dihydroxypyrimidin-5-yl)-1-hexyl phosphonic acid, a potent inhibitor of lumazine synthase.
Bioorganic & medicinal chemistry letters 1999;9(1):39-42.
1998: A B Argade; R Devraj; JA Vroman; R D Haugwitz; Melinda G Hollingshead; Mark Cushman
Design and synthesis of brefeldin A sulfide derivatives as prodrug candidates with enhanced aqueous solubilities.
Journal of medicinal chemistry 1998;41(18):3337-46.
1998: Glenda Kohlhagen; KD Paull; Mark Cushman; P Nagafuji; Yves Pommier
Protein-linked DNA strand breaks induced by NSC 314622, a novel noncamptothecin topoisomerase I poison.
Molecular pharmacology 1998;54(1):50-8.
1998: Mark Cushman; A Casimiro-Garcia; E Hejchman; JA Ruell; M Huang; CA Schaeffer; K Williamson; William G Rice; Robert W Buckheit
New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry 1998;41(12):2076-89.
1998: Mark Cushman; S Insaf; JA Ruell; CA Schaeffer; William G Rice
Synthesis of a cosalane analog with an extended polyanionic pharmacophore conferring enhanced potency as an anti-HIV agent.
Bioorganic & medicinal chemistry letters 1998;8(7):833-6.
1998: Mark Cushman; F Mavandadi; K Kugelbrey; Adelbert Bacher
Synthesis of 2,6-dioxo-(1H,3H)-9-N-ribitylpurine and 2,6-dioxo-(1H,3H)-8-aza-9-N-ribitylpurine as inhibitors of lumazine synthase and riboflavin synthase.
Bioorganic & medicinal chemistry 1998;6(4):409-15.
1998: Mark Cushman; A Casimiro-Garcia; K Williamson; William G Rice
Synthesis of a non-nucleoside reverse transcriptase inhibitor in the alkenyldiarylmethane (ADAM) series with optimized potency and therapeutic index.
Bioorganic & medicinal chemistry letters 1998;8(2):195-8.
1997: Mark Cushman; H M He; J A Katzenellenbogen; R K Varma; Ernest Hamel; C M Lin; S Ram; Y P Sachdeva
Synthesis of analogs of 2-methoxyestradiol with enhanced inhibitory effects on tubulin polymerization and cancer cell growth.
Journal of medicinal chemistry 1997;40(15):2323-34.
1996: W M Golebiewski; R F Keyes; Mark Cushman
Exploration of the effects of linker chain modifications on anti-HIV activities in a series of cosalane analogues.
Bioorganic & medicinal chemistry 1996;4(10):1637-48.
1996: R Devraj; John F Barrett; J A Fernandez; J A Katzenellenbogen; Mark Cushman
Design, synthesis, and biological evaluation of ellipticine-estradiol conjugates.
Journal of medicinal chemistry 1996;39(17):3367-74.
1996: Mark Cushman; W M Golebiewski; L Graham; Jim A Turpin; William G Rice; V Fliakas-Boltz; Robert W Buckheit
Synthesis and biological evaluation of certain alkenyldiarylmethanes as anti-HIV-1 agents which act as non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry 1996;39(16):3217-27.
1996: Johannes Scheuring; Markus Fischer; Mark Cushman; J Lee; Adelbert Bacher; H Oschkinat
NMR analysis of site-specific ligand binding in oligomeric proteins. Dynamic studies on the interaction of riboflavin synthase with trifluoromethyl-substituted intermediates.
Biochemistry 1996;35(30):9637-46.
1996: R Devraj; J Jurayj; J A Fernandez; John F Barrett; Mark Cushman
Synthesis of a series of cytotoxic 2-acyl-1,2-dihydroellipticines which inhibit topoisomerase II.
Anti-cancer drug design 1996;11(4):311-24.
1996: Adelbert Bacher; Markus Fischer; Klaus Kis; K Kugelbrey; S Mörtl; Johannes Scheuring; S Weinkauf; Sabine Eberhardt; K Schmidt-Bäse; Robert Huber; K Ritsert; Mark Cushman; Rudolf Ladenstein
Biosynthesis of riboflavin: structure and mechanism of lumazine synthase.
Biochemical Society transactions 1996;24(1):89-94.
1996: R F Keyes; W M Golebiewski; Mark Cushman
Correlation of anti-HIV potency with lipophilicity in a series of cosalane analogs having normal alkenyl and phosphodiester chains as cholestane replacements.
Journal of medicinal chemistry 1996;39(2):508-14.
1995: E Hejchman; R D Haugwitz; Mark Cushman
Synthesis and cytotoxicity of water-soluble ambrosin prodrug candidates.
Journal of medicinal chemistry 1995;38(17):3407-10.
1995: Mark Cushman; H M He; J A Katzenellenbogen; C M Lin; E Hamel
Synthesis, antitubulin and antimitotic activity, and cytotoxicity of analogs of 2-methoxyestradiol, an endogenous mammalian metabolite of estradiol that inhibits tubulin polymerization by binding to the colchicine binding site.
Journal of medicinal chemistry 1995;38(12):2041-9.
1995: Mark Cushman; W M Golebiewski; Y Pommier; A Mazumder; D Reymen; E De Clercq; L Graham; William G Rice
Cosalane analogues with enhanced potencies as inhibitors of HIV-1 protease and integrase.
Journal of medicinal chemistry 1995;38(3):443-52.
1994: Mark Cushman; H Zhu; Robert L Geahlen; A J Kraker
Synthesis and biochemical evaluation of a series of aminoflavones as potential inhibitors of protein-tyrosine kinases p56lck, EGFr, and p60v-src.
Journal of medicinal chemistry 1994;37(20):3353-62.
1994: Mark Cushman; W M Golebiewski; James B McMahon; Robert W Buckheit; D J Clanton; O Weislow; R D Haugwitz; J P Bader; L Graham; William G Rice
Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction.
Journal of medicinal chemistry 1994;37(19):3040-50.
1994: J Jurayj; R D Haugwitz; R K Varma; K D Paull; John F Barrett; Mark Cushman
Design and synthesis of ellipticinium salts and 1,2-dihydroellipticines with high selectivities against human CNS cancers in vitro.
Journal of medicinal chemistry 1994;37(14):2190-7.
1994: Johannes Scheuring; J Lee; Mark Cushman; H Patel; D A Patrick; Adelbert Bacher
(Trifluoromethyl)lumazine derivatives as 19F NMR probes for lumazine protein.
Biochemistry 1994;33(24):7634-40.
1993: K Thakkar; Robert L Geahlen; Mark Cushman
Synthesis and protein-tyrosine kinase inhibitory activity of polyhydroxylated stilbene analogues of piceatannol.
Journal of medicinal chemistry 1993;36(20):2950-5.
1993: Mark Cushman; H M He; C M Lin; E Hamel
Synthesis and evaluation of a series of benzylaniline hydrochlorides as potential cytotoxic and antimitotic agents acting by inhibition of tubulin polymerization.
Journal of medicinal chemistry 1993;36(19):2817-21.
1992: Mark Cushman; D Nagarathnam; D Gopal; H M He; C M Lin; E Hamel
Synthesis and evaluation of analogues of (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene as potential cytotoxic and antimitotic agents.
Journal of medicinal chemistry 1992;35(12):2293-306.
1992: Mark Cushman; P Sherman
Inhibition of HIV-1 integration protein by aurintricarboxylic acid monomers, monomer analogs, and polymer fractions.
Biochemical and biophysical research communications 1992;185(1):85-90.
1991: Mark Cushman; D Nagarathnam
Cytotoxicities of some flavonoid analogues.
Journal of natural products 1991;54(6):1656-60.
1991: Mark Cushman; D Nagarathnam; Robert L Geahlen
Synthesis and evaluation of hydroxylated flavones and related compounds as potential inhibitors of the protein-tyrosine kinase p56lck.
Journal of natural products 1991;54(5):1345-52.
1991: Mark Cushman; D Nagarathnam; D Gopal; A K Chakraborti; C M Lin; E Hamel
Synthesis and evaluation of stilbene and dihydrostilbene derivatives as potential anticancer agents that inhibit tubulin polymerization.
Journal of medicinal chemistry 1991;34(8):2579-88.
1991: Mark Cushman; D Nagarathnam; D L Burg; Robert L Geahlen
Synthesis and protein-tyrosine kinase inhibitory activities of flavonoid analogues.
Journal of medicinal chemistry 1991;34(2):798-806.
1991: Mark Cushman; S Kanamathareddy; E De Clercq; D Schols; M E Goldman; J A Bowen
Synthesis and anti-HIV activities of low molecular weight aurintricarboxylic acid fragments and related compounds.
Journal of medicinal chemistry 1991;34(1):337-42.
1991: Mark Cushman; P L Wang; S H Chang; C Wild; E De Clercq; D Schols; M E Goldman; J A Bowen
Preparation and anti-HIV activities of aurintricarboxylic acid fractions and analogues: direct correlation of antiviral potency with molecular weight.
Journal of medicinal chemistry 1991;34(1):329-37.
1990: Mark Cushman; P Chinnasamy; A K Chakraborti; J Jurayj; Robert L Geahlen; R D Haugwitz
Synthesis of [beta-(4-pyridyl-1-oxide)-L-alanine4]-angiotensin I as a potential suicide substrate for protein-tyrosine kinases.
International journal of peptide and protein research 1990;36(6):538-43.