Jiangsu Key Laboratory for High Technology Research of TCM Formulae, Nanjing University of Chinese Medicine, Nanjing 210046, China.
Bioorg Med Chem Lett. 2012 Oct 1;22(19):6085-8. doi: 10.1016/j.bmcl.2012.08.038. Epub 2012 Aug 16.
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.
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。