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Mark Cushman

This is a preview profile on BiomedExperts - the first literature-based scientific social network. It brings the right researchers together and allows them to collaborate online. Collexis and Dell provide the BiomedExperts network of +1.5 Million pre-calculated profiles free of charge to researchers worldwide.

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HIV-1

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Co-Publications
Name
35
Bacher, Adelbert
30
Pommier, Yves
29
Fischer, Markus
23
Antony, Smitha
22
Buckheit, Robert
18
Illarionov, Boris
15
Kohlhagen, Glenda
15
Pannecouque, Christophe
14
De Clercq, Erik
12
Hartman, Tracy
12
Morrell, Andrew
12
Turpin, Jim
10
Xiao, Xiangshu
10
Fanwick, Phillip
9
Huber, Robert

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Publications

TOP 3
Cinelli Maris A; Cordero Brenda; Dexheimer Thomas S; Pommier Yves; Cushman Mark
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
Cullen Matthew D; Ho William C; Bauman Joseph D; Das Kalyan; Arnold Eddy; Hartman Tracy L; Watson Karen M; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
Crystallographic study of a novel subnanomolar inhibitor provides insight on the binding interactions of alkenyldiarylmethanes with human immunodeficiency virus-1 reverse transcriptase.
Talukdar Arindam; Breen Meghan; Bacher Adelbert; Illarionov Boris; Fischer Markus; Georg Gunda; Ye Qi-Zhuang; Cushman Mark
Discovery and development of a small molecule library with lumazine synthase inhibitory activity.

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All Publications

2009: Cinelli Maris A; Cordero Brenda; Dexheimer Thomas S; Pommier Yves; Cushman Mark
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: Cullen Matthew D; Ho William C; Bauman Joseph D; Das Kalyan; Arnold Eddy; Hartman Tracy L; Watson Karen M; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
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: Talukdar Arindam; Breen Meghan; Bacher Adelbert; Illarionov Boris; Fischer Markus; Georg Gunda; Ye Qi-Zhuang; Cushman Mark
Discovery and development of a small molecule library with lumazine synthase inhibitory activity.
The Journal of organic chemistry 2009;74(15):5123-34.
2009: Zhao Yujie; Bacher Adelbert; Illarionov Boris; Fischer Markus; Georg Gunda; Ye Qi-Zhuang; Fanwick Phillip E; Franzblau Scott G; Wan Baojie; Cushman Mark
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: Maiti Arup; Reddy P V Narasimha; Sturdy Megan; Marler Laura; Pegan Scott D; Mesecar Andrew D; Pezzuto John M; Cushman Mark
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.
Journal of medicinal chemistry 2009;52(7):1873-84.
2009: Deng Bo-Liang; Zhao Yujie; Hartman Tracy L; Watson Karen; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
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: Yu Tsyr-Yan; O'Connor Robert D; Sivertsen Astrid C; Chiauzzi Colby; Poliks Barbara; Fischer Markus; Bacher Adelbert; Haase Ilka; Cushman Mark; Schaefer Jacob
(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: Cuendet Muriel; Oteham Carol P; Maiti Arup; Craig Bruce A; Cushman Mark; Moon Richard C; Pezzuto John M
Zapotin prevents mouse skin tumorigenesis during the stages of initiation and promotion.
Anticancer research 2008;28(6A):3705-9.
2008: Fang Zhenglai; Song Yunlong; Sarkar Taradas; Hamel Ernest; Fogler William E; Agoston Gregory E; Fanwick Phillip E; Cushman Mark
Stereoselective synthesis of 3,3-diarylacrylonitriles as tubulin polymerization inhibitors.
The Journal of organic chemistry 2008;73(11):4241-4.
2008: Cullen Matthew; Miles Deborah; Rothwell Arlene; Bonham Connie; Wood Karl V; Cushman Mark
Hydrolysis of thioesters in an ion trap.
Rapid communications in mass spectrometry : RCM 2008;22(8):1094-8.
2008: Zhang Yanlei; Illarionov Boris; Morgunova Ekaterina; Jin Guangyi; Bacher Adelbert; Fischer Markus; Ladenstein Rudolf; Cushman Mark
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: Cullen Matthew D; Cheung York-Fong; Houslay Miles D; Hartman Tracy L; Watson Karen M; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
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: Cullen Matthew D; Sarkar Taradas; Hamel Ernest; Hartman Tracy L; Watson Karen M; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
Bioorganic & medicinal chemistry letters 2008;18(2):469-73.
2007: Edsall Allison B; Agoston Gregory E; Treston Anthony M; Plum Stacy M; McClanahan Robert H; Lu Tian-Sheng; Song Wei; Cushman Mark
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: Antony Smitha; Agama Keli K; Miao Ze-Hong; Takagi Kazutaka; Wright Mollie H; Robles Ana I; Varticovski Lyuba; Nagarajan Muthukaman; Morrell Andrew; Cushman Mark; Pommier Yves
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: Cullen Matthew D; Deng Bo-Liang; Hartman Tracy L; Watson Karen M; Buckheit Robert W; Pannecouque Christophe; Clercq Erik De; Cushman Mark
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: Zhang Yanlei; Jin Guangyi; Illarionov Boris; Bacher Adelbert; Fischer Markus; Cushman Mark
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: Talukdar Arindam; Illarionov Boris; Bacher Adelbert; Fischer Markus; Cushman Mark
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: Morrell Andrew; Placzek Michael; Parmley Seth; Antony Smitha; Dexheimer Thomas S; Pommier Yves; Cushman Mark
Nitrated indenoisoquinolines as topoisomerase I inhibitors: a systematic study and optimization.
Journal of medicinal chemistry 2007;50(18):4419-30.
2007: Morrell Andrew; Placzek Michael; Parmley Seth; Grella Brian; Antony Smitha; Pommier Yves; Cushman Mark
Optimization of the indenone ring of indenoisoquinoline topoisomerase I inhibitors.
Journal of medicinal chemistry 2007;50(18):4388-404.
2007: Sakamoto Takeshi; Cullen Matthew D; Hartman Tracy L; Watson Karen M; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
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: Maiti Arup; Cuendet Muriel; Croy Vicki L; Endringer Denise C; Pezzuto John M; Cushman Mark
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: Morgunova Ekaterina; Saller Sabine; Haase Ilka; Cushman Mark; Bacher Adelbert; Fischer Markus; Ladenstein Rudolf
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: Kaiser Johannes; Illarionov Boris; Rohdich Felix; Eisenreich Wolfgang; Saller Sabine; den Brulle Jan Van; Cushman Mark; Bacher Adelbert; Fischer Markus
A high-throughput screening platform for inhibitors of the riboflavin biosynthesis pathway.
Analytical biochemistry 2007;365(1):52-61.
2007: Morrell Andrew; Placzek Michael S; Steffen Jamin D; Antony Smitha; Agama Keli; Pommier Yves; Cushman Mark
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: Zhang Yanlei; Illarionov Boris; Bacher Adelbert; Fischer Markus; Georg Gunda I; Ye Qi-Zhuang; Vander Velde David; Fanwick Phillip E; Song Yunlong; Cushman Mark
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: Kim Ha Young; Kuhn Richard J; Patkar Chinmay; Warrier Ranjit; Cushman Mark
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: Lee Chan Yong; Illarionov Boris; Woo Young-Eun; Kemter Kristina; Kim Ryu-Ryun; Eberhardt Sabine; Cushman Mark; Eisenreich Wolfgang; Fischer Markus; Bacher Adelbert
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: Maiti Arup; Cuendet Muriel; Kondratyuk Tamara; Croy Vicki L; Pezzuto John M; Cushman Mark
Synthesis and cancer chemopreventive activity of zapotin, a natural product from Casimiroa edulis.
Journal of medicinal chemistry 2007;50(2):350-5.
2006: Morrell Andrew; Antony Smitha; Kohlhagen Glenda; Pommier Yves; Cushman Mark
A systematic study of nitrated indenoisoquinolines reveals a potent topoisomerase I inhibitor.
Journal of medicinal chemistry 2006;49(26):7740-53.
2006: Nagarajan Muthukaman; Morrell Andrew; Ioanoviciu Alexandra; Antony Smitha; Kohlhagen Glenda; Agama Keli; Hollingshead Melinda; Pommier Yves; Cushman Mark
Synthesis and evaluation of indenoisoquinoline topoisomerase I inhibitors substituted with nitrogen heterocycles.
Journal of medicinal chemistry 2006;49(21):6283-9.
2006: Morgunova Ekaterina; Illarionov Boris; Sambaiah Thota; Haase Ilka; Bacher Adelbert; Cushman Mark; Fischer Markus; Ladenstein Rudolf
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: Antony Smitha; Agama Keli K; Miao Ze-Hong; Hollingshead Melinda; Holbeck Susan L; Wright Mollie H; Varticovski Lyuba; Nagarajan Muthukaman; Morrell Andrew; Cushman Mark; Pommier Yves
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: Deng Bo-Liang; Hartman Tracy L; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
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: Nagarajan Muthukaman; Morrell Andrew; Antony Smitha; Kohlhagen Glenda; Agama Keli; Pommier Yves; Ragazzon Patricia A; Garbett Nichola C; Chaires Jonathan B; Hollingshead Melinda; Cushman Mark
Synthesis and biological evaluation of bisindenoisoquinolines as topoisomerase I inhibitors.
Journal of medicinal chemistry 2006;49(17):5129-40.
2006: Morrell Andrew; Jayaraman Muthusamy; Nagarajan Muthukaman; Fox Brian M; Meckley Marintha Rae; Ioanoviciu Alexandra; Pommier Yves; Antony Smitha; Hollingshead Melinda; Cushman Mark
Evaluation of indenoisoquinoline topoisomerase I inhibitors using a hollow fiber assay.
Bioorganic & medicinal chemistry letters 2006;16(16):4395-9.
2006: Anadu Nwanne O; Davisson V Jo; Cushman Mark
Synthesis and anticancer activity of brefeldin A ester derivatives.
Journal of medicinal chemistry 2006;49(13):3897-905.
2006: Morrell Andrew; Antony Smitha; Kohlhagen Glenda; Pommier Yves; Cushman Mark
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: Deng Bo-Liang; Cullen Matthew D; Zhou Zhigang; Hartman Tracy L; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Fanwick Phillip E; Cushman Mark
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: Kim Ha Young; Talukdar Arindam; Cushman Mark
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: Marchand Christophe; Antony Smitha; Kohn Kurt W; Cushman Mark; Ioanoviciu Alexandra; Staker Bart L; Burgin Alex B; Stewart Lance; Pommier Yves
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: Xiao Xiangshu; Antony Smitha; Pommier Yves; Cushman Mark
Total synthesis and biological evaluation of 22-hydroxyacuminatine.
Journal of medicinal chemistry 2006;49(4):1408-12.
2006: Ramsperger Arne; Augustin Martin; Schott Ann-Kathrin; Gerhardt Stefan; Krojer Tobias; Eisenreich Wolfgang; Illarionov Boris; Cushman Mark; Bacher Adelbert; Huber Robert; Fischer Markus
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: Xiao Xiangshu; Cushman Mark
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: Cushman Mark; Jin Guangyi; Sambaiah Thota; Illarionov Boris; Fischer Markus; Ladenstein Rudolf; Bacher Adelbert
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: Deng Bo-Liang; Hartman Tracy L; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Fanwick Phillip E; Cushman Mark
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: Xiao Xiangshu; Cushman Mark
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: Ioanoviciu Alexandra; Antony Smitha; Pommier Yves; Staker Bart L; Stewart Lance; Cushman Mark
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: Xiao Xiangshu; Cushman Mark
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: Kim Ha Young; Patkar Chinmay; Warrier Ranjit; Kuhn Richard; Cushman Mark
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: Xiao Xiangshu; Miao Ze-Hong; Antony Smitha; Pommier Yves; Cushman Mark
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
Bioorganic & medicinal chemistry letters 2005;15(11):2795-8.
2005: Xiao Xiangshu; Antony Smitha; Pommier Yves; Cushman Mark
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: Staker Bart L; Feese Michael D; Cushman Mark; Pommier Yves; Zembower David; Stewart Lance; Burgin Alex B
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: Morgunova Ekaterina; Meining Winfried; Illarionov Boris; Haase Ilka; Jin Guangyi; Bacher Adelbert; Cushman Mark; Fischer Markus; Ladenstein Rudolf
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: Chen Jinhua; Illarionov Boris; Bacher Adelbert; Fischer Markus; Haase Ilka; Georg Gunda; Ye Qi-Zhuang; Ma Zeqiang; Cushman Mark
A high-throughput screen utilizing the fluorescence of riboflavin for identification of lumazine synthase inhibitors.
Analytical biochemistry 2005;338(1):124-30.
2005: Antony Smitha; Kohlhagen Glenda; Agama Keli; Jayaraman Muthusamy; Cao Shousong; Durrani Farukh A; Rustum Youcef M; Cushman Mark; Pommier Yves
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: Nagarajan Muthukaman; Morrell Andrew; Fort Brian C; Meckley Marintha Rae; Antony Smitha; Kohlhagen Glenda; Pommier Yves; Cushman Mark
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: Xiao Xiangshu; Antony Smitha; Kohlhagen Glenda; Pommier Yves; Cushman Mark
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: Chen Jinhua; Sambaiah Thota; Illarionov Boris; Fischer Markus; Bacher Adelbert; Cushman Mark
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: Edsall Allison B; Mohanakrishnan Arasambattu K; Yang Donglai; Fanwick Philip E; Hamel Ernest; Hanson Arthur D; Agoston Gregory E; Cushman Mark
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: Xiao Xiangshu; Antony Smitha; Kohlhagen Glenda; Pommier Yves; Cushman Mark
Design, synthesis, and biological evaluation of cytotoxic 11-aminoalkenylindenoisoquinoline and 11-diaminoalkenylindenoisoquinoline topoisomerase I inhibitors.
Bioorganic & medicinal chemistry 2004;12(19):5147-60.
2004: Koch Michael; Breithaupt Constanze; GerhardtHaase StefanIlka; Weber Stefan; Cushman Mark; Huber Robert; Bacher Adelbert; Fischer Markus
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: Morrell Andrew; Antony Smitha; Kohlhagen Glenda; Pommier Yves; Cushman Mark
Synthesis of nitrated indenoisoquinolines as topoisomerase I inhibitors.
Bioorganic & medicinal chemistry letters 2004;14(14):3659-63.
2004: Silvestri Maximilian A; Nagarajan Muthukaman; De Clercq Erik; Pannecouque Christophe; Cushman Mark
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: Cushman Mark; Sambaiah Thota; Jin Guangyi; Illarionov Boris; Fischer Markus; Bacher Adelbert
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: Fischer Markus; Schott Ann-Kathrin; Kemter Kristina; Feicht Richard; Richter Gerald; Illarionov Boris; Eisenreich Wolfgang; Gerhardt Stefan; Cushman Mark; Steinbacher Stefan; Huber Robert; Bacher Adelbert
Riboflavin synthase of Schizosaccharomyces pombe. Protein dynamics revealed by 19F NMR protein perturbation experiments.
BMC biochemistry 2003;4():18.
2003: Nagarajan Muthukaman; Xiao Xiangshu; Antony Smitha; Kohlhagen Glenda; Pommier Yves; Cushman Mark
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: Antony Smitha; Jayaraman Muthusamy; Laco Gary; Kohlhagen Glenda; Kohn Kurt W; Cushman Mark; Pommier Yves
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: Fox Brian M; Xiao Xiangshu; Antony Smitha; Kohlhagen Glenda; Pommier Yves; Staker Bart L; Stewart Lance; Cushman Mark
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: Mu Fanrong; Hamel Ernest; Lee Debbie J; Pryor Donald E; Cushman Mark
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: Zhang Xiaofeng; Meining Winfried; Cushman Mark; Haase Ilka; Fischer Markus; Bacher Adelbert; Ladenstein Rudolf
A structure-based model of the reaction catalyzed by lumazine synthase from Aquifex aeolicus.
Journal of molecular biology 2003;328(1):167-82.
2003: Fischer Markus; Haase Ilka; Kis Klaus; Meining Winfried; Ladenstein Rudolf; Cushman Mark; Schramek Nicholas; Huber Robert; Bacher Adelbert
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: Silvestri Maximilian A; Miles Deborah; Rothwell Arlene P; Wood Karl V; Cushman Mark
The 'apparent' hydrolysis of alkyl esters during electrospray ionization.
Rapid communications in mass spectrometry : RCM 2003;17(15):1703-8.
2002: Gerhardt Stefan; Schott Ann-Kathrin; Kairies Norman; Cushman Mark; Illarionov Boris; Eisenreich Wolfgang; Bacher Adelbert; Huber Robert; Steinbacher Stefan; Fischer Markus
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: Mu Fanrong; Lee Debbie J; Pryor Donald E; Hamel Ernest; Cushman Mark
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: Cushman Mark; Mohanakrishnan Arasambattu K; Hollingshead Melinda; Hamel Ernest
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: Cushman Mark; Yang Donglai; Mihalic Jeffrey T; Chen Jinhua; Gerhardt Stefan; Huber Robert; Fischer Markus; Kis Klaus; Bacher Adelbert
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: Cushman Mark; Yang Donglai; Gerhardt Stefan; Huber Robert; Fischer Markus; Kis Klaus; Bacher Adelbert
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: Xu Guozhang; Kannan Arunachalam; Hartman Tracy L; Wargo Heather; Watson Karen; Turpin Jim A; Buckheit Robert W; Johnson Allison A; Pommier Yves; Cushman Mark
Synthesis of substituted diarylmethylenepiperidines (DAMPs), a novel class of anti-HIV agents.
Bioorganic & medicinal chemistry 2002;10(8):2807-16.
2002: Gerhardt Stefan; Haase Ilka; Steinbacher Stefan; Kaiser Jens T; Cushman Mark; Bacher Adelbert; Huber Robert; Fischer Markus
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: Mehta Anil K; Studelska Daniel R; Fischer Markus; Giessauf Andreas; Kemter Kristina; Bacher Adelbert; Cushman Mark; Schaefer Jacob
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: Xu Guozhang; Hartman Tracy L; Wargo Heather; Turpin Jim A; Buckheit Robert W; Cushman Mark
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: Jayaraman Muthusamy; Fox Brian M; Hollingshead Melinda; Kohlhagen Glenda; Pommier Yves; Cushman Mark
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: Cushman M; Yang D; Kis K; Bacher A
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: Xu G; Micklatcher M; Silvestri M A; Hartman T L; Burrier J; Osterling M C; Wargo H; Turpin J A; Buckheit R W; Cushman M
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: Fox B M; Vroman J A; Fanwick P E; Cushman M
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: Casimiro-Garcia A; De Clercq E; Pannecouque C; Witvrouw M; Loftus T L; Turpin J A; Buckheit R W; Fanwick P E; Cushman M
Synthesis and anti-HIV activity of cosalane analogues incorporating two dichlorodisalicylmethane pharmacophore fragments.
Bioorganic & medicinal chemistry 2001;9(11):2827-41.
2001: Xu G; Loftus T L; Wargo H; Turpin J A; Buckheit R W; Cushman M
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: Eberhardt S; Zingler N; Kemter K; Richter G; Cushman M; Bacher A
Domain structure of riboflavin synthase.
European journal of biochemistry / FEBS 2001;268(15):4315-23.
2001: Sambaiah T; Fanwick P E; Cushman M
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: Illarionov B; Kemter K; Eberhardt S; Richter G; Cushman M; Bacher A
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: Santhosh K C; Paul G C; De Clercq E; Pannecouque C; Witvrouw M; Loftus T L; Turpin J A; Buckheit R W; Cushman M
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: Mu F; Coffing S L; Riese D J; Geahlen R L; Verdier-Pinard P; Hamel T E; Johnson J; Cushman M
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: Howard O M; Dong H F; Oppenheim J J; Insaf S; Santhosh K C; Paul G; Cushman M
Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds.
Bioorganic & medicinal chemistry letters 2001;11(1):59-62.
2000: Santhosh K C; De Clercq E; Pannecouque C; Witvrouw M; Loftus T L; Turpin J A; Buckheit R W; Cushman M
Anti-HIV activity of a series of cosalane amino acid conjugates.
Bioorganic & medicinal chemistry letters 2000;10(22):2505-8.
2000: Cushman M; Jayaraman M; Vroman J A; Fukunaga A K; Fox B M; Kohlhagen G; Strumberg D; Pommier Y
Synthesis of new indeno[1,2-c]isoquinolines: cytotoxic non-camptothecin topoisomerase I inhibitors.
Journal of medicinal chemistry 2000;43(20):3688-98.
2000: Paul G C; De Clercq E; Pannecouque C; Witvrouw M; Loftus T L; Turpin J A; Buckheit R W; Cushman M
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: Wang Z; Yang D; Mohanakrishnan A K; Fanwick P E; Nampoothiri P; Hamel E; Cushman M
Synthesis of B-ring homologated estradiol analogues that modulate tubulin polymerization and microtubule stability.
Journal of medicinal chemistry 2000;43(12):2419-29.
2000: Meining W; Mörtl S; Fischer M; Cushman M; Bacher A; Ladenstein R
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: Casimiro-Garcia A; De Clercq E; Pannecouque C; Witvrouw M; Stup T L; Turpin J A; Buckheit R W; Cushman M
Synthesis and anti-HIV activity of cosalane analogues incorporating nitrogen in the linker chain.
Bioorganic & medicinal chemistry 2000;8(1):191-200.
1999: Casimiro-Garcia A; Micklatcher M; Turpin J A; Stup T L; Watson K; Buckheit R W; Cushman M
Novel modifications in the alkenyldiarylmethane (ADAM) series of non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry 1999;42(23):4861-74.
1999: Cushman M; Insaf S; Paul G; Ruell J A; De Clercq E; Schols D; Pannecouque C; Witvrouw M; Schaeffer C A; Turpin J A; Williamson K; Rice W G
Extension of the polyanionic cosalane pharmacophore as a strategy for increasing anti-HIV potency.
Journal of medicinal chemistry 1999;42(10):1767-77.
1999: Strumberg D; Pommier Y; Paull K; Jayaraman M; Nagafuji P; Cushman M
Synthesis of cytotoxic indenoisoquinoline topoisomerase I poisons.
Journal of medicinal chemistry 1999;42(3):446-57.
1999: Cushman M; Mihalic J T; Kis K; Bacher A
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: Argade A B; Devraj R; Vroman J A; Haugwitz R D; Hollingshead M; Cushman M
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: Kohlhagen G; Paull K D; Cushman M; Nagafuji P; Pommier Y
Protein-linked DNA strand breaks induced by NSC 314622, a novel noncamptothecin topoisomerase I poison.
Molecular pharmacology 1998;54(1):50-8.
1998: Cushman M; Casimiro-Garcia A; Hejchman E; Ruell J A; Huang M; Schaeffer C A; Williamson K; Rice W G; Buckheit R W
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: Cushman M; Insaf S; Ruell J A; Schaeffer C A; Rice W G
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: Cushman M; Mavandadi F; Kugelbrey K; Bacher A
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: Cushman M; Casimiro-Garcia A; Williamson K; Rice W G
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: Cushman M; He H M; Katzenellenbogen J A; Varma R K; Hamel E; Lin C M; Ram S; Sachdeva Y P
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: Golebiewski W M; Keyes R F; Cushman M
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: Devraj R; Barrett J F; Fernandez J A; Katzenellenbogen J A; Cushman M
Design, synthesis, and biological evaluation of ellipticine-estradiol conjugates.
Journal of medicinal chemistry 1996;39(17):3367-74.
1996: Cushman M; Golebiewski W M; Graham L; Turpin J A; Rice W G; Fliakas-Boltz V; Buckheit R W
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: Scheuring J; Fischer M; Cushman M; Lee J; Bacher A; Oschkinat H
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: Devraj R; Jurayj J; Fernandez J A; Barrett J F; Cushman M
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: Bacher A; Fischer M; Kis K; Kugelbrey K; Mörtl S; Scheuring J; Weinkauf S; Eberhardt S; Schmidt-Bäse K; Huber R; Ritsert K; Cushman M; Ladenstein R
Biosynthesis of riboflavin: structure and mechanism of lumazine synthase.
Biochemical Society transactions 1996;24(1):89-94.
1996: Keyes R F; Golebiewski W M; Cushman M
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: Hejchman E; Haugwitz R D; Cushman M
Synthesis and cytotoxicity of water-soluble ambrosin prodrug candidates.
Journal of medicinal chemistry 1995;38(17):3407-10.
1995: Cushman M; He H M; Katzenellenbogen J A; Lin C M; Hamel E
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: Cushman M; Golebiewski W M; Pommier Y; Mazumder A; Reymen D; De Clercq E; Graham L; Rice W G
Cosalane analogues with enhanced potencies as inhibitors of HIV-1 protease and integrase.
Journal of medicinal chemistry 1995;38(3):443-52.
1994: Cushman M; Zhu H; Geahlen R L; Kraker A J
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: Cushman M; Golebiewski W M; McMahon J B; Buckheit R W; Clanton D J; Weislow O; Haugwitz R D; Bader J P; Graham L; Rice W G
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: Jurayj J; Haugwitz R D; Varma R K; Paull K D; Barrett J F; Cushman M
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: Scheuring J; Lee J; Cushman M; Patel H; Patrick D A; Bacher A
(Trifluoromethyl)lumazine derivatives as 19F NMR probes for lumazine protein.
Biochemistry 1994;33(24):7634-40.
1993: Thakkar K; Geahlen R L; Cushman M
Synthesis and protein-tyrosine kinase inhibitory activity of polyhydroxylated stilbene analogues of piceatannol.
Journal of medicinal chemistry 1993;36(20):2950-5.
1993: Cushman M; He H M; Lin C M; Hamel E
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: Cushman M; Nagarathnam D; Gopal D; He H M; Lin C M; Hamel E
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: Cushman M; Sherman P
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: Cushman M; Nagarathnam D
Cytotoxicities of some flavonoid analogues.
Journal of natural products 1991;54(6):1656-60.
1991: Cushman M; Nagarathnam D; Geahlen R L
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: Cushman M; Nagarathnam D; Gopal D; Chakraborti A K; Lin C M; Hamel E
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: Cushman M; Nagarathnam D; Burg D L; Geahlen R L
Synthesis and protein-tyrosine kinase inhibitory activities of flavonoid analogues.
Journal of medicinal chemistry 1991;34(2):798-806.
1991: Cushman M; Kanamathareddy S; De Clercq E; Schols D; Goldman M E; Bowen J A
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: Cushman M; Wang P L; Chang S H; Wild C; De Clercq E; Schols D; Goldman M E; Bowen J A
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: Cushman M; Chinnasamy P; Chakraborti A K; Jurayj J; Geahlen R L; Haugwitz R D
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.

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