Design, synthesis and anti-proliferative activity of novel coumarin derivatives linking Schiff base and aryl nitrogen mustard.
- Author:
Wen-Hu LIU
;
Shi-Bao WANG
;
Jin-Xia CHANG
;
Yi LIU
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
pharmacology;
Cell Line, Tumor;
Cell Proliferation;
drug effects;
Coumarins;
chemical synthesis;
pharmacology;
Drug Design;
Drug Screening Assays, Antitumor;
Humans;
Nitrogen Mustard Compounds;
chemical synthesis;
pharmacology;
Schiff Bases;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2014;49(2):217-224
- CountryChina
- Language:Chinese
-
Abstract:
To explore novel coumarin derivatives with more potent anti-proliferative activity, a series of novel compounds were designed and synthesized by linking Schiff base and N, N-bis (2-chloroethyl) amine pharmacophore of nitrogen mustards to the coumarin's framework. Their structures were confirmed by 1H NMR, MS and element analysis techniques. In vitro anti-proliferative activities were evaluated against HepG2, DU145 and MCF7 cell lines by the standard MTT assay. The results showed that some of the target compounds exhibited strong anti-proliferative activities against selected tumor cells, and compounds 7c, 7f, 7g, 7h and 7q were better than or equal to the activities of positive control, they deserved further development.
