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阿魏酸和咖啡酸衍生物的抗癌生物活性评价及构效关系分析。

Biological activity evaluation and structure-activity relationships analysis of ferulic acid and caffeic acid derivatives for anticancer.

机构信息

Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China.

出版信息

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6085-8. doi: 10.1016/j.bmcl.2012.08.038. Epub 2012 Aug 16.

Abstract

The anticancer activities of alkyl esters and NO-donors of ferulic acid (FA) and caffeic acid (CA) were assessed by a high-throughout screening (HTS) method, and the structure-activity relationships were described. CA alkyl esters had better anticancer activities than FA alkyl esters with the same alkyl substituent. Mono-nitrates and phenylfuroxan nitrates were more potent than the dual nitrates. Phenylsulfonylfuroxan nitrates of FA, especially compounds 8b-8d, exhibited more potent activities in anticancer.

摘要

通过高通量筛选(HTS)方法评估了阿魏酸(FA)和咖啡酸(CA)的烷基酯和 NO 供体的抗癌活性,并描述了它们的构效关系。具有相同烷基取代基的 CA 烷基酯比 FA 烷基酯具有更好的抗癌活性。单硝酸盐和苯并呋咱硝酸盐比双硝酸盐更有效。FA 的苯磺酰基呋咱硝酸盐,特别是化合物 8b-8d,在抗癌方面表现出更强的活性。

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