| Literature DB >> 16290932 |
Xiao-Ling Cockcroft1, Krystyna J Dillon, Lesley Dixon, Jan Drzewiecki, Frank Kerrigan, Vincent M Loh, Niall M B Martin, Keith A Menear, Graeme C M Smith.
Abstract
We have previously described the discovery of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors based on a phthalazinone scaffold. Subsequent optimisation of inhibitory activity, metabolic stability and pharmacokinetic parameters has led to a novel series of meta-substituted 4-benzyl-2H-phthalazin-1-one PARP-1 inhibitors which retain low nM cellular activity and show good stability in vivo and efficacy in cell based models.Entities:
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Year: 2005 PMID： 16290932 DOI： 10.1016/j.bmcl.2005.10.081
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823