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Chin J Nat Med. 2013 May;11(3):284-8. doi: 10.1016/S1875-5364(13)60030-8.

Synthesis and in vitro cytotoxicity evaluation of baicalein amino acid derivatives.

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  • 1Department of Natural Medicine Chemistry, China Pharmaceutical University, Nanjing, China.

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.

Copyright © 2013 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.

PMID:
23725843
[PubMed - indexed for MEDLINE]
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