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目的设计合成某些雌酮芳杂环腙类化合物,并进行体外抗肿瘤活性测试。方法以雌酮为原料,通过雌酮与水合肼反应,生成雌酮-17-肼,然后该化合物与不同的芳香醛反应,得到雌酮芳杂环腙类化合物,并采用MTT法对目标化合物进行体外抑制肿瘤细胞增殖活性实验。结果与结论设计合成了5个雌酮芳杂环腙类化合物,活性研究表明,化合物7对宫颈癌细胞He La选择性地表现出较好的抑制增殖活性,IC50值为12.1μmol·L-1(顺铂的IC50值为10.1μmol·L-1)。
Objective To design and synthesize some estrone aromatic heterocyclic hydrazones and to test the antitumor activity in vitro. Methods Estrone was used as raw material to synthesize estrone-17-hydrazine by reaction of estrone and hydrazine hydrate. Then the compound was reacted with different aromatic aldehydes to obtain estrone aromatic heterocyclic hydrazones. The target compounds In vitro inhibition of tumor cell proliferation activity experiments. RESULTS AND CONCLUSION Five estrone-bound heterocyclic hydrazones were designed and synthesized. The activity of compound 7 showed that Hela selectively inhibited the proliferation of Hela cells, with IC50 of 12.1μmol·L-1 (Cisplatin IC50 value of 10.1μmol·L-1).