Synthesis and antitumor evaluation of fluoroquinolone C3 fused heterocycles(Ⅱ):From triazolothiadiazines to pyrazolotriazoles  

作　　者：Guo Qiang Hu Li Li Hou Yong Yang Lei Yi Song Qiang Xie Guo Qiang Wang Nan Nan Duan Tie Yao Chao Xiao Yi Wen Wen Long Huang 

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

出　　处：《Chinese Chemical Letters》2011年第7期804-806,共3页中国化学快报（英文版）

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

摘　　要：To further expand an effective modified route for the shift from an antibacterial fluoroquinolone （FQ） to an antitumor FQ, two series of title compounds based on an isostere of the FQ C3 carboxylic group with two fused heterocyclic rings, [ 1,2,4]triazolo[3,4- b][1,3,4]thiadiazine and pyrazolo[5,1-c][1,2,4]triazole, respectively, were designed and synthesized starting from the current antibacterial FQs, and their in vitro antitumor activity against L1210, CHO cell lines were evaluated via their respective IC50 values.To further expand an effective modified route for the shift from an antibacterial fluoroquinolone （FQ） to an antitumor FQ, two series of title compounds based on an isostere of the FQ C3 carboxylic group with two fused heterocyclic rings, [ 1,2,4]triazolo[3,4- b][1,3,4]thiadiazine and pyrazolo[5,1-c][1,2,4]triazole, respectively, were designed and synthesized starting from the current antibacterial FQs, and their in vitro antitumor activity against L1210, CHO cell lines were evaluated via their respective IC50 values.

关 键 词：FLUOROQUINOLONE Triazolothiadiazine Pyrazolotriazole Antitumor evaluation 

分 类 号：O626[理学—有机化学] S859.796[理学—化学]