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摘要：
Inspired by the significant anti-cancer activity of our previously screened natural ergosterol peroxide (EP, 1), we synthesized and characterized a series of novel 5 alpha,8 alpha-epidioxyandrost-3 beta-ol-17-(O-phenylacetamide)oxime derivatives (9a-o). The anti-proliferative activity of the synthesized compounds against human hepatocellular carcinoma cells (HepG2, Sk-Hep1) and human breast cancer cells (MCF-7, MDA-MB231) were investigated. Compounds 9d, 9f, 9h, 9j and 9m displayed good anti-proliferative activity (most IC50 ＜ 20 mu M) in vitro. Furthermore, fluorescence imaging showed that the designed coumarin-9d conjugate (12) localized mainly in mitochondria, leading to enhanced anticancer activities over the parent structure. (C) 2017 Elsevier Ltd. All rights reserved.
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来源 ：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN： 0960-894X
年份： 2017
期： 16
卷： 27
页码： 3856-3861
2 . 7 0 0
JCR@2022
ESI学科： CHEMISTRY;
ESI高被引阀值：127
中科院分区：3
