具有去甲斑蝥素结构的HDAC抑制剂的设计与合成

摘要

Objective To design and synthesize the histone deacetylase inhibitors with norcantharidian.Methods By combining nor-cantharidian with benzamide derivatives we synthesized 2 novel compounds.Results The structures of the novel target compounds were confirmed by MS,1 H-NMR and 13 C-NMR.Conclusion The easily controlled,gentle way to synthesize the series of compounds is worked out.%目的：设计与合成以去甲斑蝥素为骨架的苯甲酰胺类组蛋白去乙酰化酶抑制剂。方法利用拼合原理，将去甲斑蝥素的活性结构片段，引入具有不同取代基的苯甲酰胺类组蛋白去乙酰化酶抑制剂中，探索性设计并合成了2个未经报道的全新化合物。结果目标化合物为全新未报道化合物，结构经质谱、氢谱和碳谱确认。结论设计思想合理，合成方法温和，简便，适合该类化合物的合成。