Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 16, Pages 3739-3743Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.07.001
Keywords
PARP-1 inhibitor; 4-(Thiophen-2-ylmethyl)-2H-phthalazin-1-ones; Synthesis; Biological evaluation; Antitumor
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Funding
- Major Program of Ministry of Science and Technology of China [2013ZX09J13103]
- National Natural Science Foundation of China [81102309]
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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. (C) 2014 Elsevier Ltd. All rights reserved.
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