title: Synthesis and in vitro cytotoxicity evaluation of baicalein amino acid derivatives.
abstract: OBJECTIVE
  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.
  
  
  CONCLUSIONS
  Compounds 4c, 4d, 7a and 7b showed a significant increase in cytotoxicity compared with baicalein.
authors.affiliation: Department of Natural Medicine Chemistry, China Pharmaceutical University, Nanjing, China.
authors.forename: Lei
authors.initials: L
authors.lastname: Li
authors.forename: Wen-Yuan
authors.initials: WY
authors.lastname: Liu
authors.forename: Feng
authors.initials: F
authors.lastname: Feng
authors.forename: Chun-Yong
authors.initials: CY
authors.lastname: Wu
authors.forename: Ning
authors.initials: N
authors.lastname: Xie
mesh_terms: D000215:Acylation; D000596:Amino Acids / Q000737:chemistry*; D049109:Cell Proliferation / Q000187:drug effects; D044950:Flavanones / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D056945:Hep G2 Cells; D006801:Humans; D008745:Methylation; D015394:Molecular Structure
chemical_list: D000596:Amino Acids; D044950:Flavanones; C006680:baicalein