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Bioorg Med Chem Lett. 2005 May 2;15(9):2235-8.

Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.

Author information

1
KuDOS Horsham Ltd, 26 Foundry Lane, Horsham, West Sussex RH13 5PX, UK. vloh@kudospharma.co.uk

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.

PMID:
15837300
DOI:
10.1016/j.bmcl.2005.03.026
[Indexed for MEDLINE]

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