📜2-Hydroxy-3-Oxo-Ursa-1,12-Dien-28-Oic Acid置于sodium Tetrahydroborate体系中,用 四氢呋喃,甲醇 作为反应溶剂,化学反应 1.0H,以3.7 G的收率获得产物2Beta-羟基熊果酸
参考文献:Urea Derivates Of Ursolic,Oleanolic And Maslinic Acid Induce Apoptosis And Are Selective Cytotoxic For Several Human Tumor Cell Lines
标题:Urea Derivates Of Ursolic,Oleanolic And Maslinic Acid Induce Apoptosis And Are Selective Cytotoxic For Several Human Tumor Cell Lines
摘要:2,3-Di-O-Acetyl-Maslinic Acid Benzylamide (5) Has Previously Been Shown To Possess High Cytotoxicity For A Variety Of Human Tumor Cell Lines While Being Of Low Cytotoxicity To Non-Malignant Cells. Structural Modifications Performed On 5 Revealed That The Presence Of These Acetyl Groups In 5 And The Presence Of (2 Beta,3 Beta)-Configurated Centers Seems Necessary For Obtaining High Cytotoxicity Combined With Best Selectivity Between Malignant Cells And Non-Malignant Mouse Fibroblasts. Compounds Carrying An Ursane Skeleton Showed Weaker Cytotoxicity Than Their Oleanane Derived Analogs. In Addition,The Benzylamide Function In Compound 5 Should Be Replaced By A Phenylurea Moiety To Gain Better Cytotoxicity While Retaining And Improving The Selectivity. Thus,Maslinic Acid Derived N-[2 Beta,3 Beta-Di-O-Acetyl-17 Beta-Amino-28-Norolean-12-En-17-Yliphenylurea (45) Gave Best Results Showing Ec50 = 0.9 Mu M (For A2780 Ovarian Cancer Cells) With Ec50 > 120 Mu M For Fibroblasts (Nih 3T3) And Triggered Apoptosis While Caspase-3 Was Not Activated By This Compound. (C) 2016 Elsevier Masson Sas. All Rights Reserved.
DOI:10.1016/j.Ejmech.2016.04.051