Synthesis and in vitro cytotoxicity evaluation of baicalein amino acid derivatives

AimTo synthesize the baicalein amino acid derivatives and evaluate their cytotoxicity activities in vitro.MethodsAmino 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.ResultsThirteen novel derivatives were synthesized and characterized. Their cytotoxic activities were assessed by the MTT method on the inhibition of HepG2 cells in vitro.ConclusionCompounds 4c, 4d, 7a and 7b showed a significant increase in cytotoxicity compared with baicalein.