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目的发现由抗菌氟喹诺酮转化为抗肿瘤氟喹诺酮的有效结构修饰方法。方法均三唑杂环作为氧氟沙星(1)C-3羧基的等排体,功能基硫乙酰腙类及腙类为其杂环排体的修饰基团,设计合成了氟喹诺酮C-3均三唑硫乙酰腙类及C-3均三唑腙类目标化合物。用四唑盐(MTT)方法评价了目标化合物对体外培养肿瘤细胞的生长抑制活性。结果合成了14个目标化合物,体外均显示潜在的抗肿瘤活性,有意义的是腙类目标化合物的活性强于酰腙类化合物活性。结论均三唑腙结构作为C-3羧基的等排体有利于提高其抗肿瘤活性。
OBJECTIVE: To find an effective method for the structural modification of anti-tumor fluoroquinolones by antibacterial fluoroquinolones. Methods The triazole heterocycles were designed as the isosteres of the carboxyl group ofloxacin (1) C-3, functional thioacetyl hydrazones and hydrazones as the heterocyclic groups. The fluoroquinolone C- 3-triazole thioacetyl hydrazones and C-3 are triazole hydrazone target compounds. The growth inhibitory activity of the target compound on cultured tumor cells was evaluated by the tetrazolium salt (MTT) method. Results 14 target compounds were synthesized and showed potential antitumor activity in vitro. It is significant that the hydrazone target compounds are more active than the acylhydrazone compounds. Conclusion The isothiazolylhydrazone structure is an isostere of C-3 carboxyl group, which is helpful to improve its anti-tumor activity.