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

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

Volume: 9 Issue: 7

Author(s): Yi Bi, Jinyi Xu, Fei Sun, Xiaoming Wu, Wencai Ye, Yijun Sun and Wenwen Huang

Affiliation:

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

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.

Cite this article as:

Bi Yi, Xu Jinyi, Sun Fei, Wu Xiaoming, Ye Wencai, Sun Yijun and Huang Wenwen, Synthesis and Biological Activity of 28-Amide Derivatives of 23-Hydroxy Betulinic Acid as Antitumor Agent Candidates, Medicinal Chemistry 2013; 9 (7) . https://dx.doi.org/10.2174/1573406411309070005