酰胺类NO供体熊果酸衍生物的合成

Synthesis of Amide NO-Donating Ursolic Acid Derivatives

为提高五环三萜类天然产物熊果酸的抗肿瘤活性,以熊果酸为母核引入具有广泛生物活性的酰胺结构以及具有抗肿瘤作用的NO供体支链形成酰胺类NO供体型熊果酸衍生物。采用熊果酸为原料,经氧化、亲核取代等多步反应合成8个酰胺类NO供体熊果酸衍生物2、12~18,所有化合物采用IR、^1H NMR、^13C NMR、HR MS进行表征。

A pentacyclic triterpenoid was derived from nature to improve the antitumor effect of ursolic acid,.The amide structure with broad biological activity and anti-tumor NO donor branches were combined with ursolic acid to form amide NO donor ursolic acid derivatives by using ursolic acid as starting material.Eight amide NO donor ursolic acid derivatives 2、12~18 were synthesized through oxidation and nucleophilic substitution.All structures of derivatives were confirmed by IR,^1H NMR,^13C NMR and HR MS.