Discovery of potent poly (ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone
Jagtap, P.G, Baloglu, E, Southan, G.J, Mabley, J.G, Li, H.S, Zhou, J, Van Duxer, J, Salzman, A.L and Szabo, C (2005) Discovery of potent poly (ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone Journal of Medicinal Chemistry, 48 (16). pp. 5100-5103. ISSN 0022-2623
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Official URL: http://dx.doi.org/10.1021/jm0502891
Novel indeno[1,2-c]isoquinolinone derivatives were synthesized and evaluated as inhibitors of the nuclear enzyme poly(ADP-ribose) polymerase-1 (PARP-1). These potent nonmutagenic PARP-1 inhibitors possess an additional five-membered ring between the B and C rings of 6(5H)-phenanthridinone. The most potent PARP-1 inhibitors were obtained from the substitution of the D ring at the C-9 position, in particular sulfonamide and N-acyl analogues (6 and 11). The 9-sulfonamide analogues 11a and 12a exhibited IC50 values of 1 and 10 nM, respectively.
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