| Literature DB >> 15837300 |
Vincent M Loh1, Xiao-ling Cockcroft, Krystyna J Dillon, Lesley Dixon, Jan Drzewiecki, Penny J Eversley, Sylvie Gomez, Janet Hoare, Frank Kerrigan, Ian T W Matthews, Keith A Menear, Niall M B Martin, Roger F Newton, Jane Paul, Graeme C M Smith, Julia Vile, Alan J Whittle.
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.Entities:
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Year: 2005 PMID： 15837300 DOI： 10.1016/j.bmcl.2005.03.026
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823