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为寻找具有抗肿瘤活性的新型组蛋白去乙酰化酶(HDAC)抑制剂,在前期研究发现活性结构A和B的基础上,设计合成了N-(2-氨基-4-吡啶)苯甲酰胺类(A类)化合物和N-(2-氨基-3-吡啶)苯甲酰胺类(B类)化合物各16个。32个目标化合物的结构经1HNMR及HR-MS分析确证。体外抑HDACs活性研究表明,除Ⅴ-20、Ⅴ-21外,其余30个化合物在200μmol·L-1下均表现出一定的抑酶活性。对各肿瘤细胞株的体外抗增殖作用研究表明,化合物Ⅴ-30、Ⅴ-31、Ⅴ-32对Hut78、Jurkat E6-1、A549、K562及MDA-MB-435s5种肿瘤细胞具有良好的抑制活性。
In order to find a novel histone deacetylase (HDAC) inhibitor with antitumor activity, based on the previous studies on the active structures A and B, N- (2-amino-4-pyridyl) benzamide Sixteen each of compounds of the Class A (Class A) and N- (2-amino-3-pyridyl) benzamides (Class B) The structures of 32 target compounds were confirmed by 1HNMR and HR-MS analyzes. Inhibition of HDACs in vitro showed that except for Ⅴ-20 and Ⅴ-21, the other 30 compounds showed some inhibitory activity at 200μmol·L-1. The in vitro anti-proliferative effects of all the tumor cell lines showed that compounds V-30, V-31 and V-32 had good inhibitory activity against 5 kinds of Hut78, Jurkat E6-1, A549, K562 and MDA-MB-435s tumor cells .