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靶向组蛋白去乙酰化酶新型化合物的体外抗肿瘤活性筛选
  • 期刊名称:解放军药学学报,2009. 26(6):482-486
  • 时间:0
  • 分类:R914.5[医药卫生—药物化学;医药卫生—药学]
  • 作者机构:[1]安徽医科大学,合肥230032, [2]军事医学科学院放射与辐射医学研究所,北京100850
  • 相关基金:国家自然科学基金(30772628)资助
  • 相关项目:新型抗肿瘤药物HDAC抑制剂苯甲酰胺类衍生物的设计、合成及构效关系研究
中文摘要:

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.

英文摘要:

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.

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