Synthesis and in vitro cytotoxicity evaluation of baicalein amino acid derivatives

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 1H 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.