Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 48, Issue 16, Pages 5100-5103Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm0502891
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Funding
- NIDDK NIH HHS [R44 DK 054099] Funding Source: Medline
- NIGMS NIH HHS [R44 GM 058986] Funding Source: Medline
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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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