Synthesis and cytotoxicity evaluation of oleanolic acid derivatives

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• 作者：Jia Hao^a ; ^b ; Jun Liu^c ; Xiaoan Wen^b ; ^{wxagj@126.com} ; Hongbin Sun^b ; ^{hbsun2000@yahoo.com}
• 关键词：LTIPWULUUZXUOW-OYSMALFBSA-N ; XYVFHJQDCQIOST-QJWBNFRSSA-N ; MEYQFEZHZUWOAH-FBWKWWTKSA-N ; XDXUVETWXWCTFM-BEUHLGRCSA-N
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：1 April, 2013
• 年：2013
• 卷：23
• 期：7
• 页码：2074-2077
• 全文大小：1014 K

文摘

Twelve derivatives of oleanolic acid (boldFont"">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 boldFont"">17 exhibited the most potent cytotoxicity against PC3 cell line (IC₅₀ = 0.39 ¦ÌM) and compound boldFont"">28 displayed the best activity against A549 cell line (IC₅₀ = 0.22 ¦ÌM). 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.