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Indexed by:期刊论文

Date of Publication:2010-05-01

Journal:BIOORGANIC & MEDICINAL CHEMISTRY

Included Journals:SCIE、PubMed、Scopus

Volume:18

Issue:9

Page Number:3279-3284

ISSN No.:0968-0896

Key Words:Benzo[c,d]indol-2(1H)-one; Antitumor agents; DNA intercalator; DNA cleavage

Abstract:Several 2-(substituted benzo[c,d]indol-2(1H)-ylidene) malononitriles have been designed and synthesized. Their DNA binding, antitumor and DNA damaging properties were evaluated. All the compounds exhibited efficient antitumor activities with preference to be against the tumor cell line 7721 rather than the tumor cell line MCF-7. Compound 1f could intercalate into DNA entirely presumably by the good conjugation of carbonyl group with benzo[c,d] indol moiety. What's more, 1f exhibited potent toxicity against MCF-7 cells with IC(50) at 0.003 mu M and against 7721 cells at 0.115 mu M, respectively. (C) 2010 Elsevier Ltd. All rights reserved.