以MS-275为先导化合物,设计并合成8个苯甲酰胺类组蛋白去乙酰化酶抑制剂,其结构经MS与1H-NMR确证.以MS-275为阳性对照药物,测试8个目标化合物对人乳腺癌细胞MCF-7和人肺癌细胞A549的体外抗肿瘤细胞增殖活性,结果显示,合成的8个目标化合物中有6个化合物表现出较好的抑制肿瘤的活性,尤其是化合物5a与7b对肿瘤细胞的体外抑制活性与MS-275相比有较为显著地提高,可为进一步研究提供参考.
MS-275 was taken as the lead compound, eight benzamides as histone deacetylase inhibitor were de- signed and synthesized, and their structures were identified by MS and ^1H-NMR. A test of target compounds on hu- man breast cancer ceils MCF-7 and human lung cancer cells A549 in vitro antiproliferative activity has been done, in which MS-275 was taken as a positive control. The results showed that six compounds of target compounds showed better tumor suppression activity, especially the vitro inhibitory activity on tumor cells of compounds 5a and 7b has a more remarkably improved compared with the MS-275,they can be mentioned for further study as reference.