85999-41-3Relevant academic research and scientific papers
Synthesis and biological evaluation of ambradiolic acid as an inhibitor of glycogen phosphorylase
Liu, Jie,Zhang, Hengyuan,Zhu, Peiqing,Wu, Xiaoming,Yao, Hequan,Ye, Wencai,Jiang, Jieyun,Xu, Jinyi
, p. 50 - 55 (2015)
Ambradiolic acid (3) with oleanane skeleton is a natural pentacyclictriterpene. The first synthesis of 3 starting from 23-hydroxybetulinic acid (2) has been accomplished in 12-steps with a total yield of 18.1% in our study. Compound 3 was further biologically evaluated and found to exhibit significant inhibitory activity against rabbit muscle glycogen phosphorylase (GP) with an IC50 value of 12.4 μM, suggesting it could be a potential lead compound for the development of hypoglycemic drugs.
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
experimental part, 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.
Terpenoids. III: Synthesis and biological evaluation of 23-hydroxybetulinic acid derivatives as novel inhibitors of glycogen phosphorylase
Zhu, Peiqing,Bi, Yi,Xu, Jinyi,Li, Zan,Liu, Jun,Zhang, Luyong,Ye, Wencai,Wu, Xiaoming
body text, p. 6966 - 6969 (2010/06/19)
A series of 23-hydroxybetulinic acid derivatives were prepared and tested in vitro as a new class of inhibitors of glycogen phosphorylase (GP). Within this series of compounds, 12b (IC50 = 3.5 μM) is the most potent GPa inhibitor. The preliminary SAR results of the 23-hydroxybetulinic acid derivatives are discussed.
NMDA AND MC RECEPTOR ANTAGONISTS EXHIBITING NEUROPROTECTIVE AND MEMORY ENHANCING ACTIVITIES
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Page/Page column 38-39, (2009/01/20)
The present invention provides therapeutically active compounds and compositions as NMDA and MC receptor antagonists, which are useful in preventing and treating central nervous system disorders by inhibiting over-activation of NMDA and/or MC receptors. In one aspect, the present invention provides methods of treating and/or preventing neurodegenerative diseases and neuropathological disorders, methods of providing neuroprotection under stress conditions such as a stroke, methods of enhancing the brain's cognitive functions and methods of treating depression, anxiety and cachexia induced by a chronic disease in mammals and humans.
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.
