中文摘要：

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。

英文摘要：

OBJECTIVE To explore an efficient modification strategy for conversion of antibacterial fluoroquinolones to antitumor ones. METHODS An azole heterocyclic ring,s-triazole,as a bioisotere of the C-3 carboxylic acid for ofloxacin（ 1）,functional acylhydrazones and hydrazones,was used as the modified side-chain for the C-3 bioisotere,then the C-3 s-triazole acylhydrazones and s-triazole hydrazone derivatives were designed and their in vitro antitumor activity was evaluated by MTT assay. RESULTS Fourteen target compounds were synthesized,and they exhibited stronger antitumor activity than the parent ofloxacin. And most importantly,hydrazone derivatives had higher activity than their corresponding acylhydrazone compounds. CONCLUSION s-Triazole-hydrazone moiety is warranted special attention as an efficient bioisosteric replacement of the C-3 carboxylic acid for further development of antitumor fluoroquinolone lead compounds.