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

Acta Pharmaceutica Sinica B

Wen-Long Huang¹  Lei Yi²  Nan-nan Duan²  Guo-qiang Hu²  Guo-qiang Wang²  Tie-yao Cao²  Xiao-yi Wen²  Song-qiang Xie²  Yong Yang² 

[1] Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China;Institute of Chemistry & Biology, Henan University, Kaifeng 475001, China;

关键词: Fluoroquinolone;    Triazolothiadiazole;    Synthesis;    Antitumor evaluation;   

DOI  :  10.1016/j.apsb.2011.07.001

来源: DOAJ

【 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.

【 授权许可】

Unknown