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以去氢表雄酮为原料,通过微波一步合成法及常规2步合成方法合成得到16个新的具有不同结构特征的去氢表雄酮噻唑衍生物.所有合成物都通过了IR、NMR及HRMS的结构表征.另外,分别选用人宫颈癌细胞(He La)、人肝癌细胞(Hep G)、人肺癌细胞(A549)和人正常肾上皮细胞(HEK-293T)对合成物的抗肿瘤活性进行了研究,结果表明4-(4’-三氟甲基)苯基噻唑-2-去氢表雄酮腙(4)对所测试的肿瘤细胞株具有很好的生长增殖抑制活性,对上述肿瘤细胞的IC_(50)值分别为13.2、11.3和8.3μmol·L~(-1),对人肾上皮正常细胞HEK-293T却没有表现出明显的抑制作用(IC_(50)值>100μmol·L~(-1)).但是,其它合成物对所测试的细胞株没有表现出明显的抑制活性.
Using dehydroepiandrosterone as raw material, 16 new dehydroepiandrosterone thiazole derivatives with different structural characteristics were synthesized by microwave one-step synthesis and conventional 2-step synthesis.All the compounds were characterized by IR, NMR and HRMS was used to characterize the antitumor activity of the composite.Moreover, the antitumor activity of Hela, HepG, A549 and HEK-293T were also evaluated. The results showed that 4- (4’-trifluoromethyl) phenylthiazole-2-dehydroepiandrosterone hydrazone (4) had a good growth-inhibitory activity against the tumor cell strains tested, The IC 50 values of tumor cells were 13.2, 11.3 and 8.3 μmol·L -1, respectively, but no significant inhibition was found on HEK-293T cells (IC 50> 100 μmol · L -1 However, other compounds did not show significant inhibitory activity on the cell lines tested.