Design,Synthesis and Antitumor Activity of Fluoroquinolone C3 Heterocyclic Bis-oxadiazole Methylsulfide Derivatives Derived from Levofloxacin

作     者：HU Guo-qlang WANG Guo-qiang DUAN Nan-nan WEN Xiao-yi CAO Tie-yao XIE Song-qiang HUANG Wen-long 

作者机构：Institute of Pharmacy Henan University Kaifeng 475001 P. R. China Centre of Drug Discovery China Pharmaceutical University Nanjing 210009 P. R. China 

基　　金：Supported by the National Natural Science Foundation of China(Nos.20872028 21072045) 

出 版 物：《Chemical Research in Chinese Universities》 (高等学校化学研究（英文版）)

年 卷 期：2012年第28卷第6期

页      码：980-984页

摘      要：To discover an efficient route for the shift from an antibacterial fluoroquinolone to an antitumor one based on the mechanistic similarities between targeting topoisomerases and the eukaryotic ones,two series of the title compounds,C3 bis-oxadiazole methylsulfides 6a―6h and corresponding dimethylpiperazinium iodides 7a―7h derived from levofloxacin 1 were designed and *** in vitro antiproliferative activities against Chinese hamster ovary cell line（CHO）,murine leukemia cell line（L1210） and human leukocytoma cell line（HL60） were evaluated by MTT assay,and inhibitory effect on DNA topoisomerase IIα was also measured by means of densitometric assay.

主 题 词：Fluoroquinolone Oxadiazole Isostere Sulfide Piperazinium Antitumor activity 

学科分类：090603[090603] 0710[理学-生物科学类] 071010[071010] 081704[081704] 07[理学] 08[工学] 0817[工学-轻工类] 09[农学] 0906[农学-水产类] 

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