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中文摘要：
目的 发现转化抗菌氟喹诺酮到抗肿瘤氟喹诺酮的有效途径。方法 氧氟沙星酰肼与芳香羧酸在三氯氧磷中缩环合到目标物2-氟喹诺酮-5-芳基-NFDE6二唑衍生物。用MTT方法评价目标化合物3对体外培养肿瘤细胞的生长抑制活性。结果 合成了10个新的目标化合物,体外均显示潜在的抗癌活性。结论 杂环用作羧基的等排体值得关注。
英文摘要：
ObjectiveTo discover an efficient route for the conversion of an antibacterial fluoroquinolone to an antitumor one. Methods Cyclo-condensation of ofloxacin hydrazide 2 with aromatic carboxylic acids in POCl3 gave the corresponding oxadiazole derivatives 3a-3j, and their antitumor activity was evaluated by MTT assay. Results Ten title compunds were synthesized and showed potential antitumor activity. Conclusion Heterocycles as isosteric replacement of carboxyl are warrant further development.
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同项目期刊论文
Part II: Design, synthesis and antitumor action of C3/C3 bis-fluoroquinolones linked-cross 2,5-[1,3,
Synthesis and antitumor evaluation of fluoroquinolone C3 fused heterocycles (II): From triazolothiad
Design, synthesis and antitumor activity of C3/C3 bis- fluoroquinolones cross-linked with [1,2,4]tri
Synthesis and antitumor evaluation of C3/C3 fluoroquinolone dimmers (I): Tethered with a fused heter
Design, synthesis and antitumor activity of C-3/C-3 bis-fluoroquinolones cross-linked with [1,24]tri
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