952479-68-4Relevant academic research and scientific papers
Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors
Scarpelli, Rita,Boueres, Julia K.,Cerretani, Mauro,Ferrigno, Federica,Ontoria, Jesus M.,Rowley, Michael,Schultz-Fademrecht, Carsten,Toniatti, Carlo,Jones, Philip
scheme or table, p. 488 - 492 (2010/04/26)
A potent series of substituted 2-phenyl-2H-indazole-7-carboxamides were synthesized and evaluated as inhibitors of poly (ADP-ribose) polymerase (PARP). This extensive SAR exploration culminated with the identification of substituted 5-fluoro-2-phenyl-2H-indazole-7-carboxamide analog 48 which displayed excellent PARP enzyme inhibition with IC50 = 4 nM, inhibited proliferation of cancer cell lines deficient in BRCA-1 with CC50 = 42 nM and showed encouraging pharmacokinetic properties in rats compared to the lead 6.
AMIDE SUBSTITUTED INDAZOLE AND BENZOTRIAZOLE DERIVATIVES AS POLY(ADP-RIBOSE)POLYMERASE (PARP) INHIBITORS
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Page/Page column 79, (2008/06/13)
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly (ADP-ribose) polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusio
