| Literature DB >> 12408707 |
Stacie S Canan Koch1, Lars H Thoresen, Jayashree G Tikhe, Karen A Maegley, Robert J Almassy, Jianke Li, Xiao-Hong Yu, Scott E Zook, Robert A Kumpf, Cathy Zhang, Theodore J Boritzki, Rena N Mansour, Kanyin E Zhang, Anne Ekker, Chris R Calabrese, Nicola J Curtin, Suzanne Kyle, Huw D Thomas, Lan-Zhen Wang, A Hilary Calvert, Bernard T Golding, Roger J Griffin, David R Newell, Stephen E Webber, Zdenek Hostomsky.
Abstract
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-6-ones and 3,4-dihydropyrrolo[4,3,2-de]isoquinolin-5-(1H)-ones, have conformationally locked benzamide cores that specifically interact with the PARP-1 protein. The compounds have been evaluated with in vitro cellular assays that measure the ability of the PARP-1 inhibitors to enhance the effect of cytotoxic agents against cancer cell lines.Entities:
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Year: 2002 PMID： 12408707 DOI： 10.1021/jm020259n
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446