Synthesis and cytotoxicity evaluation of oleanolic acid derivatives.

Jia Hao, Jun Liu, Xiaoan Wen, Hongbin Sun

Tianjin Key Laboratory of Phytochemistry and Pharmaceutical Analysis, Tianjin University of Traditional Chinese Medicine, Tianjin 300193, PR China.

Bioorganic & medicinal chemistry letters 2013 Apr 1

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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. Copyright © 2013 Elsevier Ltd. All rights reserved.

Citation

Jia Hao, Jun Liu, Xiaoan Wen, Hongbin Sun. Synthesis and cytotoxicity evaluation of oleanolic acid derivatives. Bioorganic & medicinal chemistry letters. 2013 Apr 1;23(7):2074-7