期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 22, 页码 5377-5383出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.09.027
关键词
Isoflavene; Phenoxodiol; Anti-cancer; Mannich base; Benzoxazine
资金
- University of New South Wales
- Australian Research Council
Phenoxodiol, an analogue of the isoflavone natural product daidzein, is a potent anti-cancer agent that has been investigated for the treatment of hormone dependent cancers. This molecular scaffold was reacted with different primary amines and secondary amines under different Mannich conditions to yield either benzoxazine or aminomethyl substituted analogues. These processes enabled the generation of a diverse range of analogues that were required for structure-activity relationship (SAR) studies. The resulting Mannich bases exhibited prominent anti-proliferative effects against SHEP neuroblastoma and MDA-MB-231 breast adenocarcinoma cell lines. Further cytotoxicity studies against MRC-5 normal lung fibroblast cells showed that the isoflavene analogues were selective towards cancer cells. (C) 2015 Elsevier Ltd. All rights reserved.
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