Literature DB >> 25086680

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

Ling-xiao Wang1, Xin-bo Zhou1, Meng-liang Xiao1, Ning Jiang2, Feng Liu2, Wen-xia Zhou2, Xiao-kui Wang3, Zhi-bing Zheng4, Song Li1.   

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.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  4-(Thiophen-2-ylmethyl)-2H-phthalazin-1-ones; Antitumor; Biological evaluation; PARP-1 inhibitor; Synthesis

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Substances：

Year:  2014        PMID： 25086680     DOI： 10.1016/j.bmcl.2014.07.001

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

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Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

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Journal:  J Med Chem       Date:  2021-08-03       Impact factor: 8.039
  5 in total

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