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论文类型：期刊论文

发表时间：2009-01-15

发表刊物：BIOORGANIC & MEDICINAL CHEMISTRY

收录刊物：SCIE、PubMed、Scopus

卷号：17

期号：2

页面范围：804-810

ISSN号：0968-0896

关键字：Amonafide analogues; Coupling reaction; DNA-binding

摘要：A series of 5-alkylamino substituted amonafide analogues were synthesized from naphthalic anhydride by three steps including bromization, amination and CuI/proline catalyzed coupling reaction. The CuI/L-proline catalyzed coupling reaction was first applied to the naphthalimide system. These new amonafide analogues showed potential anticancer activities against HeLa and P388D1 cell lines in vitro, and 4a, 4b, and 4h exhibited better activity than amonafide against HeLa cell under the same experimental conditions. More importantly, the new analogues could avoid the side effect of amonafide due to their structure, in which lacks a primary amine at the 5 position. Moreover, the DNA-binding of the analogues was also investigated. (C) 2009 Published by Elsevier Ltd.