Synthesis and cytotoxicity evaluation of oleanolic acid derivatives |
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| Authors: | Jia Hao Jun Liu Xiaoan Wen Hongbin Sun |
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| Institution: | 1. Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, PR China;2. State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China;3. Jiangsu Center for Drug Screening, China Pharmaceutical University, 1 Shennonglu, Nanjing 210038, PR China |
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| Abstract: | Twelve derivatives of oleanolic acid (1) have been synthesized and evaluated for their inhibitory activities against the growth of prostate PC3, breast MCF-7, lung A549, and gastric BGC-823 cancer cells by MTT assays. Within these series of derivatives, compound 17 exhibited the most potent cytotoxicity against PC3 cell line (IC50 = 0.39 μM) and compound 28 displayed the best activity against A549 cell line (IC50 = 0.22 μM). SAR analysis indicates that H-donor substitution at C-3 position of oleanolic acid may be advantageous for improvement of cytotoxicity against PC3, A549 and MCF-7 cell lines. |
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