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目的为发现抗菌氟喹诺酮向抗肿瘤活性转化的有效修饰策略。方法以均三唑为氧氟沙星C-3羧基的等排体、通过缩环合反应设计了C-3噻二唑并均三唑稠杂环目标化合物(5a~5l,6a~6l)。用元素分析和光谱数据确证化合物的结构,用MTT方法评价了目标化合物对体外培养的SMMC-7721、Capan-1和HL60 3种癌细胞株的抗增值活性。结果合成了12个新型结构的C-3稠杂环目标化合物,体外抗肿瘤活性强于母体1和相应中间体硫醚酮5的活性,但弱于硫醚酮缩氨基硫脲化合物6的活性。结论 C-3稠杂环等排体的结构修饰值得进一步研究。
The purpose is to find effective antifungal fluoroquinolones conversion of anti-tumor activity of the modified strategy. Methods The target compounds (5a ~ 5l, 6a ~ 6l) of C-3 thiadiazole and homostyrazole fused heterocycle were designed by the condensation reaction of the homostriazole, which is an isostere of C-3 carboxyl ofloxacin. . The structure of the compounds was confirmed by elemental analysis and spectroscopic data. The anti-proliferation activity of the target compounds against the three cancer cell lines SMMC-7721, Capan-1 and HL60 cultured in vitro was evaluated by MTT method. Results Twelve novel C-3 fused heterocycles targeting compounds were synthesized and their anti-tumor activity in vitro was stronger than those of parent 1 and corresponding intermediate thioether-ketone 5, but weaker than the activity of thioether-thiosemicarbazone compound 6 . Conclusion Structural modifications of C-3 fused heterocyclic isostructures deserve further study.