1402463-79-9Relevant academic research and scientific papers
Synthesis, characterization, and biological studies of diosgenyl analogs
Huang, Bao-Zhan,Xin, Guang,Ma, Li-Mei,Wei, Ze-Liang,Shen, Yan,Zhang, Rui,Zheng, Hua-Jie,Zhang, Xiang-Hua,Niu, Hai,Huang, Wen
, p. 272 - 298 (2017)
A series of diosgenyl analogs were prepared from diosgenin to evaluate their anticancer activity and antithrombotic property. Analog 4, which had a spiroketal structure with a 6-aminohexanoic acid residue, exhibited the highest potency against all five tumor cell lines. It significantly blocked tumor growth, induced cell apoptosis and autophagy, and regulated cellular calcium concentration, mitochondrial membrane potential, adenosine triphosphate, and cell cycle. In addition, fluorescence-tagged compounds indicated that the analogs could rapidly accumulate in the cytoplasm, but no specific localization in the nucleus of cancer cells was observed. Furthermore, preliminary structure–activity relationship studies demonstrated that spiroketal analogs exhibit better antithrombotic activity than furostanic analogs, which exhibit the opposite effect by promoting thrombosis. Our study indicates that compound 4 may be a promising anticancer drug candidate for cancer patients with thromboembolism.
Diosgenin-3-derivative as well as preparation method and application thereof
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, (2018/03/26)
The invention relates to a diosgenin-3-derivative as well as a preparation method and application thereof. The diosgenin-3-derivative shown as a formula I provided by the invention has a structural formula shown in the description, wherein R1 is amino straight-chain fatty acid residue or amino acid residue; R2 is H or a structural formula shown in the description; R3 is H, C1-C18 alkyl or phenyl.The derivative disclosed by the invention is rich in raw material source, simple and convenient in synthetic route, high in yield and suitable for large-scale production; the derivative has excellentantitumor activity and is superior to diosgenin.
Synthesis, characterization and biological studies of diosgenyl analogues
Huang, Baozhan,Du, Dan,Zhang, Rui,Wu, Xiaohua,Xing, Zhihua,He, Yang,Huang, Wen
, p. 7330 - 7334 (2013/02/23)
A series of optical amino acid diosgenyl esters and diosgenyl salicylate conjugates were designed and synthesized to develop new anticancer and anti-inflammatory agents. The analogue 9c that contains an 6-aminohexanoic acid residue at C-3 of diosgenin exhibits higher potency against all three tumor cell lines with IC50 values ranging from 4.7 μM in C26 cells to 14.6 μM in Hep G2 cells. In addition, seven of newly synthesized compounds significantly inhibit xylene-induced ear edema and exhibit comparable or better anti-inflammatory activities than those of diosgenin and aspirin. Furthermore, preliminary structure-activity relationship studies demonstrate that diosgenyl salicylate conjugates have stronger anti-inflammatory activities than amino acid diosgenyl esters.
