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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.
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
URL: http://dx.doi.org/10.1021/jm020259n
DOI: 10.1021/jm020259n
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