期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 85, 期 -, 页码 487-497出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.07.076
关键词
Xanthone; Synthesis; Anticancer activity; Structure-activity relationships; Apoptosis; Intracellular calcium; Mitochondrial membrane potential
资金
- National Natural Science Foundation of China [21002015]
- Natural Science Foundation of Guangxi [2010GXNSFB013013, 2012GXNSFCB053001]
- Foundation of Guangxi Medicine Personnel Highlands [1107]
- Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University), Ministry of Education of the People's Republic of China [07109001-14, CMEMR2014-A01]
A series of novel 1-hydroxyl-3-aminoalkoxy xanthone derivatives were designed, synthesized and evaluated for in vitro anticancer activity against four selected human cancer cell lines (nasopharyngeal neoplasm CNE, liver cancer BEL-7402, gastric cancer MGC-803, lung adenocarcinoma A549). Most of the synthesized compounds exhibit effective cytotoxic activity against the four tested cancer cell lines with the IC50 values at micromolar concentration level. Some preliminary structure activity relationships were also discussed. In this series of derivatives, compound 3g shows excellent broad spectrum anticancer activity with IC50 values ranging from 3.57 to 20.07 mu M. The in vitro anticancer activity effect and action mechanism of compound 3g on human gastric carcinoma MGC-803 cell were further investigated. The results showed that compound 3g exhibits dose- and time-dependent anticancer effects on MGC-803 cells through apoptosis, which might be associated with its decreasing intracellular calcium and the mitochondrial membrane potential. (C) 2014 Elsevier Masson SAS. All rights reserved.
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