Novel Tricyclic Poly(ADP-ribose) Polymerase-1 Inhibitors with Potent Anticancer Chemopotentiating Activity: Design, Synthesis, and X-ray Cocrystal Structure
Journal of Medicinal Chemistry2002Vol. 45(23), pp. 4961–4974
Citations Over TimeTop 10% of 2002 papers
Stacie S. Canan Koch, Lars Thoresen, Jayashree Tikhe, Karen A. Maegley, Robert J. Almassy, Jianke Li, Xiaohong 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, Zdeněk Hostomský
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.
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