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Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis, and X-ray cocrystal structure

Lookup NU author(s): Dr Christopher Calabrese, Professor Nicola CurtinORCiD, Suzanne Kyle, Huw ThomasORCiD, Lan Wang, Professor Alan Calvert, Emeritus Professor Bernard Golding, Professor Roger Griffin, Professor Herbie Newell


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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-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.

Publication metadata

Author(s): Koch SSC, Thoresen LH, Tikhe JG, Maegley KA, Almassy RJ, Li JK, Yu XH, Zook SE, Kumpf RA, Zhang C, Boritzki TJ, Mansour RN, Zhang KE, Ekker A, Calabrese CR, Curtin NJ, Kyle S, Thomas HD, Wang LZ, Calvert AH, Golding BT, Griffin RJ, Newell DR, Webber SE, Hostomsky Z

Publication type: Article

Publication status: Published

Journal: Journal of Medicinal Chemistry

Year: 2002

Volume: 45

Issue: 23

Pages: 4961-4974

ISSN (print): 0022-2623

ISSN (electronic): 1520-4804


DOI: 10.1021/jm020259n


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