Design, synthesis and antitumor activity of valproic acid salicylanilide esters.
- Author:
Ming YUAN
1
;
Jia-Ming LI
;
Guang-Wei HE
;
Guo-Chen ZHONG
;
Yan-Chun ZHANG
Author Information
1. Department of Pharmacy, AnHui University of Chinese Medicine, AnHui Key Laboratory of Traditional Chinese Medicine, Hefei 230031, China.
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
chemistry;
pharmacology;
Cell Line, Tumor;
Cell Proliferation;
drug effects;
Drug Design;
Esters;
Humans;
Inhibitory Concentration 50;
K562 Cells;
Molecular Structure;
Prodrugs;
chemical synthesis;
chemistry;
pharmacology;
Salicylanilides;
chemical synthesis;
chemistry;
pharmacology;
Structure-Activity Relationship;
Valproic Acid;
chemical synthesis;
chemistry;
pharmacology
- From:
Acta Pharmaceutica Sinica
2013;48(6):874-880
- CountryChina
- Language:Chinese
-
Abstract:
A series of valproic acid salicylanilide esters were designed and synthesized based on the principle of prodrug. The structures of the target compounds were confirmed by MS, 1H NMR and 13C NMR. Anti-tumor activities of these compounds against K562, A549, A431 cells in vitro were investigated by MTT assay and SRB assay. The results indicated that the compounds 6h-6j were found to have stronger cell growth inhibitory action than gefitinib, and comparable to niclosamide, which are worth to be intensively studied further.
