Synthesis and Biological Activity of 28-Amide Derivatives of 23-Hydroxy Betulinic Acid as Antitumor Agent Candidates

Yi      Bi; Jinyi      Xu; Fei      Sun; Xiaoming      Wu; Wencai      Ye; Yijun      Sun; Wenwen      Huang

doi:10.2174/1573406411309070005

Abstract

Based on the structure of 23-hydroxybetulinic acid (1), a series of 28-amide derivatives were synthesized. Biological evaluation in vitro for their antitumor activities against five cell lines (A549, BEL-7402, SF-763, B16 and HL-60) has indicated that compound 6g possesses the most effective antitumor activity with an IC₅₀ value of 10.47 μM when treated with HL-60 cells. In vivo testing has also shown a comparable activity of 6g to cyclophosphamide against H22 liver tumor in mice and 5-fluorouracil against B16 melanoma, respectively.

Keywords: 23-hydroxy betulinic acid, 28-carboxylic acid, amide derivatives, antitumor activity.

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