期刊
CHEMMEDCHEM
卷 12, 期 6, 页码 466-474出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201700021
关键词
carbamates; coumarins; ergosterol peroxide; fluorescence imaging; mitochondria
资金
- Chinese Natural Science Foundation [21272020]
- Beijing Key Laboratory for Green Catalysis and Separation
Inspired by the significant anticancer activity of our previously screened natural ergosterol peroxide (1), we synthesized and characterized a series of novel ergosterol peroxide 3-carbamate derivatives. The antiproliferative activities of the synthesized compounds against human hepatocellular carcinoma cells (HepG2, SK-Hep1) and human breast cancer cells (MCF-7, MDA-MB231) were investigated. 5 alpha,8 alpha-Epidioxyergosta-3-yl-(piperazine-1)carbamate (3d) and 5 alpha,8 alpha-epidioxyergosta-3-yl-(piperidin-4-methylamine)carbamate (3f) and their hydrochloride salts exhibited significant invitro antiproliferative activities against the tested tumor cell lines, with IC50 values ranging from 0.85 to 4.62 mu m. Furthermore, fluorescent imaging showed that the designed coumarin-3d conjugate (5) localized mainly in mitochondria, leading to enhanced anticancer activities over the parent structure 1. As a whole, it appeared that substituent changes at the C3 position could serve as a promising launch point for further design of this type of steroidal anticancer agent.
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