Synthesis and in vitro cytotoxicity evaluation of baicalein amino acid derivatives.
10.1016/S1875-5364(13)60030-8
- Author:
Lei LI
1
;
Wen-Yuan LIU
;
Feng FENG
;
Chun-Yong WU
;
Ning XIE
Author Information
1. Department of Natural Medicine Chemistry, China Pharmaceutical University, Nanjing, China.
- Publication Type:Journal Article
- MeSH:
Acylation;
Amino Acids;
chemistry;
Cell Proliferation;
drug effects;
Flavanones;
chemical synthesis;
chemistry;
toxicity;
Hep G2 Cells;
Humans;
Methylation;
Molecular Structure
- From:
Chinese Journal of Natural Medicines (English Ed.)
2013;11(3):284-288
- CountryChina
- Language:English
-
Abstract:
AIM:To synthesize the baicalein amino acid derivatives and evaluate their cytotoxicity activities in vitro.
METHODS:Amino acids were subjected to methylation and aminoacylation reaction, then reacted with formaldehyde and baicalein to synthesize baicalein-8 benzyl amino acid derivatives. Through carboxyl group protection and aminoacylation of amino acid and benzyl protection of baicalein, derivatives of baicalein-6-O-amino acid esters were obtained. All of the target compounds were identified by IR, MS and (1)H NMR.
RESULTS:Thirteen novel derivatives were synthesized and characterized. Their cytotoxic activities were assessed by the MTT method on the inhibition of HepG2 cells in vitro.
CONCLUSION:Compounds 4c, 4d, 7a and 7b showed a significant increase in cytotoxicity compared with baicalein.
