Synthesis and cytotoxicity evaluation of oleanolic acid derivatives
Synthesis and cytotoxicity evaluation of oleanolic acid derivatives
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齐墩果酸衍生物的合成及细胞毒性评价
DOI：
10.1016/j.bmcl.2013.01.129
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发表时间：
2013-04-01
影响因子：
2.7
通讯作者：
Sun, Hongbin
中科院分区：
文献类型：
--
作者：
Hao, Jia;Liu, Jun;Sun, Hongbin
合成了12种油酸衍生物（1），并通过MU试验评价了它们对前列腺癌PC 3、乳腺癌MCF-7、肺癌A549和胃癌BGC-823细胞生长的抑制活性。在这些系列衍生物中，化合物17对PC 3细胞系显示出最强的细胞毒性（IC 50 = 0.39 μ M），化合物28对A549细胞系显示出最好的活性（IC 50 = 0.22 μ M）。SAR分析表明，在油酸的C-3位的H-供体取代可能有利于提高对PC 3，A549和MCF-7细胞系的细胞毒性。(C)2013爱思唯尔有限公司保留所有权利。
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 MU assays. Within these series of derivatives, compound 17 exhibited the most potent cytotoxicity against PC3 cell line (IC50 = 0.39 mu M) and compound 28 displayed the best activity against A549 cell line (IC50 = 0.22 mu M). 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. (C) 2013 Elsevier Ltd. All rights reserved.