抗肿瘤氟喹诺酮C-3(稠)杂环化合物2-氟喹诺酮-5-芳基-噁二唑衍生物的合成(Ⅱ)  

Synthesis and Antitumor Activity of Fluoroquinolone C-3 Heterocycles-Oxadiazole Derivatives(Ⅱ)

作　　者：侯莉莉[1] 银俊[1] 王伟[1] 谢松强[1] 黄文龙[2] 胡国强[1] 

机构地区：[1]河南大学化学生物学研究所,河南开封475004 [2]中国药科大学,南京210009

出　　处：《中国药学杂志》2013年第14期1194-1196,共3页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(20872028,21072045);河南大学科研基金资助

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-噁二唑衍生物。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。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.

关 键 词：抗肿瘤氟喹诺酮 噁二唑 生物等排体 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学]