Synthesis and biological evaluation of substituted 4-(thiophen-2-ylmethyl)-2H-phthalazin-1-ones as potent PARP-1 inhibitors.

Abstract:

:We have developed a series of substituted 4-(thiophen-2-ylmethyl)-2H-phthalazin-1-ones as potent PARP-1 inhibitors. Preliminary biological evaluation indicated that most compounds possessed inhibitory potencies comparable to, or higher than AZD-2281. Among these compounds, 18q appeared to be the most notable one, which displayed an 8-fold improvement in enzymatic activity compared to AZD-2281. These efforts lay the foundation for our further investigation.

journal_name

Bioorg Med Chem Lett

authors

Wang LX,Zhou XB,Xiao ML,Jiang N,Liu F,Zhou WX,Wang XK,Zheng ZB,Li S

doi

10.1016/j.bmcl.2014.07.001

subject

Has Abstract

pub_date

2014-08-15 00:00:00

pages

3739-43

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)00725-2

journal_volume

24

pub_type

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