916139-48-5Relevant academic research and scientific papers
Synthesis and biological activity of 28-amide derivatives of 23-hydroxy betulinic acid as antitumor agent candidates
Bi, Yi,Xu, Jinyi,Sun, Fei,Wu, Xiaoming,Ye, Wencai,Sun, Yijun,Huang, Wenwen
, p. 920 - 925 (2014/01/06)
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 10.47μM 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.
Synthesis and biological activity of 23-hydroxybetulinic acid c-28 ester derivatives as antitumor agent candidates
Bi, Yi,Xu, Jinyi,Sun, Fei,Wu, Xiaoming,Ye, Wencai,Sun, Yijun,Huang, Wenwen
, p. 8832 - 8841 (2012/11/13)
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 IC50 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.
Synthesis and antiproliferative evaluation of 23-hydroxybetulinic acid derivatives
Lan, Ping,Wang, Jiao,Zhang, Dong-Mei,Shu, Chang,Cao, Hui-Hui,Sun, Ping-Hua,Wu, Xiao-Ming,Ye, Wen-Cai,Chen, Wei-Min
, p. 2490 - 2502 (2011/06/24)
Based on structural modifications of the natural 23-hydroxybetulinic acid, a series of novel its derivatives had been synthesized. The new compounds were screened for in vitro antiproliferative activity against cancer cell lines HeLa, MCF-7, HepG2, B16 and A375 using doxorubicin as a reference. The vast majority of derivatives had exhibited potent tumor growth inhibitory activity than original compound. The derivatives 4, 5, 7, 20, 23, 26, 43 and 44 with IC 50 values lower than 10 μM on all tested cell lines were regarded as the most promising compounds. The structure-activity relationships of 23-hydroxybetulinic acid derivatives were also discussed in the present investigations.
Synthesis and cytotoxic activity of 17-carboxylic acid modified 23-hydroxy betulinic acid ester derivatives
Bi, Yi,Xu, Jinyi,Wu, Xiaoming,Ye, Wencai,Yuan, Shengtao,Zhang, Luyong
, p. 1475 - 1478 (2007/10/03)
New 17-carboxylic acid modified 23-hydroxy betulinic acid ester derivatives were prepared and tested for cytotoxic activity on five cancer cell lines in vitro: all tested compounds showed stronger cytotoxic activity than 23-hydroxy betulinic acid and betulinic acid. In addition, compound 5a was tested for anti-tumor activity in vivo: it had much better anti-tumor activity than 23-OH betulinic acid and had similar anti-tumor activity with cyclophosphamide and 5-fluorouracil.
