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 non-mutagenic 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.
Original language | English (US) |
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Pages (from-to) | 5100-5103 |
Number of pages | 4 |
Journal | Journal of medicinal chemistry |
Volume | 48 |
Issue number | 16 |
DOIs | |
State | Published - Aug 11 2005 |
Externally published | Yes |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery