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1HMNR、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。
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.