- Synthesis and biological activity of 23-hydroxybetulinic acid C-28 ester derivatives as antitumor agent candidates.
Synthesis and biological activity of 23-hydroxybetulinic acid C-28 ester derivatives as antitumor agent candidates.
Molecules (Basel, Switzerland) (2012-07-27)
Yi Bi, Jinyi Xu, Fei Sun, Xiaoming Wu, Wencai Ye, Yijun Sun, Wenwen Huang
PMID22832884
ABSTRACT
23-Hydroxybetulinic acid (1) served as the precursor for the synthesis of C-28 ester derivatives. The target compounds were evaluated in vitro for their antitumor activities against five cell lines (A549, BEL-7402, SF-763, B16 and HL-60). Among the obtained compounds, 6i had the most potent antitumor activity, with the IC(50 values of 8.35 µM in HL-60 cells and showed similar antitumor activity as cyclophosphamide in H22 liver tumor and as 5-fluorouracil in B16 melanoma in vivo.
MATERIALS