期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 6, 页码 2490-2502出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.03.038
关键词
23-Hydroxybetulinic acid; Structural modification; Antiproliferative activity; Structure-activity relationship
资金
- Natural Science Foundation of Guangdong Province [9151063201000053]
- Program for Changjiang Scholars and Innovative Research Team in University [IRT0965]
- Science and Technology Program of China [2009ZX09103-313]
- Guangzhou City Research Plan [2009A1-E011-1]
Based on structural modifications of the natural 23-hydroxybetulinic acid, a series of novel its derivatives had been synthesized. The new compounds were screened for in vitro antiproliferative activity against cancer cell lines HeLa, MCF-7, HepG2. B16 and A375 using doxorubicin as a reference. The vast majority of derivatives had exhibited potent tumor growth inhibitory activity than original compound. The derivatives 4, 5, 7, 20, 23, 26, 43 and 44 with IC50 values lower than 10 mu M on all tested cell lines were regarded as the most promising compounds. The structure activity relationships of 23-hydroxybetulinic acid derivatives were also discussed in the present investigations. (C) 2011 Elsevier Masson SAS. All rights reserved.
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