氧代固醇衍生物的合成及其抗癌活性研究

Studies on the synthesis and antitumor activities of oxysterol derivatives

目的合成新型氧代固醇衍生物并对其抗癌活性进行研究。方法以胆甾烷 3β ,5α ,6 β 三醇为原料合成氧代固醇琥珀酸单酯的一乙醇胺盐系列化合物 ;以各种含羟基固醇化合物为原料 ,分别与正丁酰氯等反应合成氧代固醇的正丁酸酯系列化合物。并对这两类化合物进行了体外抗癌活性试验。结果与结论共合成 13个未见文献报道的氧代固醇类化合物 ,结构经IR、1H NMR以及元素分析得到确证 ,初步体外药理试验表明 :化合物 4具有很好的抗癌活性。

Aim To design and synthesize new type of oxysterols and evaluate their antitumor activities.Methods The ethanol amine salts of hemisuccinate of some oxysterols and oxysterol butyrates were synthesized.The structures were confirmed through the methods of IR, 1H-NMR and elemental analysis.Their antitumor activities were tested in vitro.Results Thirteen unknown compounds were synthesized.Conclusion Compound 4 exhibited excellent antitumor activity in vitro.