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Bioorg Med Chem Lett
; 15(9): 2235-8, 2005 May 02.
Article
in English
| MEDLINE
| ID: mdl-15837300
ABSTRACT
Screening of the Maybridge compound collection identified 4-arylphthalazinones as micromolar inhibitors of PARP-1 catalytic activity. Subsequent optimisation of both inhibitory activity and metabolic stability led to a novel series of meta-substituted 4-benzyl-2H-phthalazin-1-ones with low nanomolar, cellular activity as PARP-1 inhibitors and promising metabolic stability in vitro.