Synthesis and antitumor evaluation of sophocarpine-cinnamic acid ester derivatives as potential antitumor agents
10.7501/j.issn.0253-2670.2019.04.006
- Author:
Dong-Chun WANG
1
Author Information
1. Center of Research and Development on Life Sciences and Environmental Sciences, Harbin University of Commerce
- Publication Type:Journal Article
- Keywords:
Antitumor activity;
Cinnamic acid;
Sophocarpine;
Structural modification;
Structure-activity relationship
- From:
Chinese Traditional and Herbal Drugs
2019;50(4):821-828
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To synthesize sophocarpine-cinnamic acid ester derivatives and evaluate the in vitro antitumor activities of the derivatives. Methods: Taking sophocarpine as the starting material, the target compounds were synthesized by oxidation, esterification, N-alkylation, reduction, condensation, hydrolysis, and salification. Their antitumor activities in vitro were evaluated for HeLa, HepG2 and A-549 by MTT assay. Results: Eleven sophocarpine-cinnamic acid ester derivatives were synthesized and the structures were characterized by 1H-NMR, 13C-NMR and HRMS. MTT assay showed that some derivatives exhibited good antitumor activities. Compound 5g showed good antitumor activity against three human tumor cell lines, which was better than that of the positive control drug, cisplatin. Conclusion: Some derivatives showed promising antitumor activities and compound 5g was worth further studying.
