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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Loh VM Jr,Cockcroft XL,Dillon KJ,Dixon L,Drzewiecki J,Eversley PJ,Gomez S,Hoare J,Kerrigan F,Matthews IT,Menear KA,Martin NM,Newton RF,Paul J,Smith GC,Vile J,Whittle AJ

doi

10.1016/j.bmcl.2005.03.026

subject

Has Abstract

pub_date

2005-05-02 00:00:00

pages

2235-8

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00332-X

journal_volume

15

pub_type

杂志文章

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