新型组蛋白去乙酰化酶抑制剂的合成及抗肿瘤活性研究

Synthesis and activity of some new histone deacetylases inhibitors

摘要:
为寻找新型组蛋白去乙酰化酶抑制剂, 设计合成了酰胺类、脲类和酰肼类全新结构类型的12个目标化合物, 并测定了体外HDAC酶抑制活性。目标化合物的结构经¹H MNR、元素分析及MS分析确证。体外HDAC酶抑制活性评价结果表明, 化合物Ia的抑酶活性较好, 值得进一步研究, 化合物IIa、IIb、IIIa～IIIi具有一定的抑酶活性。

Abstract:
To explore novel histone deacetylase (HDAC) inhibitors with anti-tumor activity, twelve target compounds were synthesized, and their structures were confirmed by ¹H NMR, MS and elemental analyses. Evaluation results in vitro showed that compound Ia exhibited potent inhibition against HDAC and is worth for further investigation. And compounds IIa, IIb, IIIa−IIIi possessed moderate HDAC inhibitory activity.