- Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis, and X-ray cocrystal structure
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A series of novel compounds have been designed that are potent inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1), and the activity and physical properties have been characterized. The new structural classes, 3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol
- Canan Koch, Stacie S.,Thoresen, Lars H.,Tikhe, Jayashree G.,Maegley, Karen A.,Almassy, Robert J.,Li, Jianke,Yu, Xiao-Hong,Zook, Scott E.,Kumpf, Robert A.,Zhang, Cathy,Boritzki, Theodore J.,Mansour, Rena N.,Zhang, Kanyin E.,Ekker, Anne,Calabrese, Chris R.,Curtin, Nicola J.,Kyle, Suzanne,Thomas, Huw D.,Wang, Lan-Zhen,Calvert, A. Hilary,Golding, Bernard T.,Griffin, Roger J.,Newell, David R.,Webber, Stephen E.,Hostomsky, Zdenek
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p. 4961 - 4974
(2007/10/03)
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- Tricyclic inhibitors of poly(ADP-ribose) polymerases
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Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapuetics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and nuerodegenerative disease. STR1As cancer therapuetics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.
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