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Synthesis and antitumor evaluation of fluoroquinolone C3 fused heterocycles(Ⅱ):From triazolothiadiazines to pyrazolotriazoles
作者姓名: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
作者单位:a Institute of Chemistry & Biology, Henan University, Kaifeng 475001, China;b China Pharmaceutical University, Nanjing 210009, China
基金项目: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]triazolo3,4- b]1,3,4]thiadiazine and pyrazolo5,1-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
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