Part II: Design, synthesis and antitumor action of C3/C3 bisfluoroquinolones linked-cross 2, 5-1, 3, 4oxadiazole.
- Author:
Guo-qiang HU
1
;
Yong YANG
;
Lei YI
;
Xin WANG
;
Zhi-qiang ZHANG
;
Song-qiang XIE
;
Wen-long HUANG
Author Information
1. Institute of Chemistry & Biology, Henan University, Kaifeng 475001, China. hgqxy@sina.com.cn
- Publication Type:Journal Article
- MeSH:
Animals;
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
CHO Cells;
drug effects;
Cell Line, Tumor;
Cricetinae;
Cricetulus;
Drug Design;
Fluoroquinolones;
chemical synthesis;
chemistry;
pharmacology;
HL-60 Cells;
drug effects;
Humans;
Inhibitory Concentration 50;
Leukemia L1210;
pathology;
Molecular Structure;
Oxadiazoles;
chemical synthesis;
chemistry;
pharmacology;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2010;45(8):1012-1016
- CountryChina
- Language:English
-
Abstract:
To develop a new small molecular probe for discovering an antitumor lead compound from the replacement of carboxylic group of two molecular antibacterial fluoroquinolones with a heterocyclic ring, a series of the C3/C3 bis-fluoroquinolones tethered with an 1, 3, 4-oxadiazole ring were synthesized as their respective HCl salts, and their structures were characterized by elemental analysis and spectral data. The in vitro antitumor activity against L1210, CHO and HL60 cell lines was also evaluated via the respective IC50 values by methylthiazole trazolium (MTT) assay.
