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 Duzer, 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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Abstract

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.

Item Type: Journal article
Subjects: C000 Biological and Biomedical Sciences
DOI (a stable link to the resource): 10.1021/jm0502891
Faculties: Faculty of Science and Engineering > School of Pharmacy and Biomolecular Sciences > Disease Process > Diabetes
Depositing User: editor spbs
Date Deposited: 08 Nov 2007
Last Modified: 08 Jul 2013 15:05
URI: http://eprints.brighton.ac.uk/id/eprint/3082

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