中文摘要：

目的寻找抗菌氟喹诺酮转化为抗肿瘤活性的c3羧基有效生物电子等排体。方法均三唑杂环作为抗菌氟喹诺酮氧氟沙星（1）c3羧基的等排体，用畦二唑作为修饰杂环，设计合成了C3双异杂环均三唑嗯二唑甲硫醚目标化合物，6-氟-7-（4-甲基哌嗪-1-基）l，8-（2，1-氧丙基）-3-[5-（5-芳基-[1，3，4]-喂二唑-2-甲硫基）4矾[1，2，4]-三唑-3-基]-喹啉-4（1H）-酮（6a～6j），用噻唑蓝（MTT）方法评价其体外抗肿瘤活性。结果合成了10个新双异杂环硫醚目标化合物，体外抗肿瘤活性显著高于母体化合物氧氟沙星的活性。结论均三唑杂环可作为c-3羧基的有效等排体。

英文摘要：

ABJECTIVE To explore an efficient heterocyclic bioisostere as the C3 carhoxylic group of antibacterial fluoroquinolo- nes for further development of antitumor fluoroquinolones. METHODS Using the s-triazole ring as an isosteric replacement of the C3 carboxylic group with another different heteroeyelic ring, oxadiazole, as a modified group, new his-（ different azole）methylsulfide deriva- tives, 6-fluoro-7- （4-methyl-piperazin- 1 -yl） -1,8- （ 2,1 -oxpropyl ） -5- [ 5- （ aryl- [ 1,3,4 ] -oxadiazol- 2-methylsulfanyl ） -4H- [ 1,2,4 ] -tri- azol-3yl] -quinolin-4 （IH） -ones （ 6a - 6j ） , were designed from ofloxacin （ 1 ）. The in vitro antitumor activity of 6a - 6j against three cancer cell lines was evaluated by MTT assay. RESULTS Ten title compounds （6a -6j）were synthesized and their structures were characterized by spectral data. They exhibited significantly higher in vitro antitumor potency than the parent compound ofloxacin. CONCLUSION The heterocyclic ring,s-triazole, could be used as an efficient isostere of the C-3 earboxylie group for further develop- ment of antitumor fluoroquinolone candidates.