Synthesis and in vitro cytotoxicity evaluation of baicalein amino acid derivatives

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.