Design, synthesis and antitumor activity of C3/C3 bis-fluoroquonolones cross-linked with [1,2,4]triazolo[3,4-b] [1,3,4]thiadiazole
| Autor: | 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 |
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| Jazyk: | angličtina |
| Rok vydání: | 2011 |
| Předmět: | |
| Zdroj: | Acta Pharmaceutica Sinica B, Vol 1, Iss 3, Pp 172-177 (2011) |
| Druh dokumentu: | article |
| ISSN: | 2211-3835 2211-3843 |
| DOI: | 10.1016/j.apsb.2011.07.001 |
| Popis: | 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. |
| Databáze: | Directory of Open Access Journals |
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