Design, synthesis and antitumor activity of C3/C3 bis-fluoroquonolones cross-linked with [1,2,4]triazolo[3,4-b] [1,3,4]thiadiazole  

作　　者：Guo-qiang Hu Yong Yang Lei Yi Guo-qiang Wang Nan-nan Duan Xiao-yi Wen Tie-yao Cao Song-qiang Xie Wen-Long Huang 

机构地区：[1]Institute of Chemistry&Biology,Henan University,Kaifeng 475001,China [2]Center of Drug Discovery,China Pharmaceutical University,Nanjing 210009,China

出　　处：《Acta Pharmaceutica Sinica B》2011年第3期172-177,共6页药学学报（英文版）

基　　金：supported by the National Natural Science Foundation of China(nos.20872028,21072045).

摘　　要：To contribute to the development of an efficient method for the conversion of antibacterial fluoroquinolones to antitumor fluoroquinolones,a series of C3/C3 bis-fluoroquinolone fused heterocycles cross-linked with a[1,2,4]-triazolo[3,4-b][1,3,4]-thiadiazole core as a common bioisostere of two carboxylic acid groups was designed and synthesized as their hydrochloride salts.Structures were characterized by elemental analysis and spectral data and their in vitro antitumor activity against L1210,CHO and HL60 cell lines was screened by determination of their IC50 values in the methylthiazole trazolium(MTT)assay.Two compounds were highly potent against the HL60 cell line and represent promising lead compounds for future development.

关 键 词：FLUOROQUINOLONE Triazolothiadiazole SYNTHESIS Antitumor evaluation 

分 类 号：O62[理学—有机化学]