Synthesis and Antitumor Activity of 17-carboxylic acid Modified Amide Derivatives of 23-hydroxy betulinic acid

Yi Bi; Jin-Yi Xu; Fei Sun; Xiao-Ming Wu; Wen-Cai Ye; Yi-Jun Sun; Qing-Guo Meng; Wen-Wen Huang
October 2013
Records of Natural Products;Oct2013, Vol. 7 Issue 4, p254
Academic Journal
A novel series of 17-carboxylic acid modified amide derivatives of 23-hydroxy betulinic acid (1) were prepared and tested in vitro against five cell lines: A549 (human lung carcinoma), BEL-7402 (human hepatoma), SF-763 (human cerebroma), B16 (mice melanoma) and HL-60 (human leukaemia). Within this series of compounds, 4a (IC50 =21.08 µM in SF-763, IC50=21.63 µM in HL-60), 4b (IC50=28.45 µM in HL-60,IC50=29.32 µM in BEL-7402 ) and 6g (IC50=26.09 µM in BEL-7402, IC50=22.65 µM in HL-60) have the more potent cytotoxic activity than lead compound 1. The preliminary structure-activity relationship analysis of the C-28 amide derivatives is also discussed.


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