摘要/Abstract

从睾酮出发，经过3-羰基肟化、Beckmann重排反应构建A-环甾体内酰胺甾核骨架，并以此为母体对17-羟基进行官能团改造与结构修饰，引入一些杂环基团，合成了一些结构新颖的A-Homo甾体内酰胺噻唑衍生物.通过IR、NMR及HRMS等现代分析方法对化合物进行了结构表征，并对化合物进行体外抑制肿瘤细胞生长增殖活性测试，结果表明其中某些化合物对所测试肿瘤细胞具有明显的抑制活性，但对人正常肾上皮细胞没有明显的抑制作用.
关键词: 睾酮, 甾体杂环化合物, A-Homo甾体内酰胺噻唑衍生物, 抗肿瘤活性
Using a testosterone as a raw material, a steroidal skelecton with A-homo-lactam was constructed. Then, some new aza-A-homocholesteryl-lactam thiazole derivatives were synthesized by modifying of the 17-hydroxyl and introducing of various heterocycles, and their structures were determined by IR, NMR and HRMS. The antiproliferative activity of the compounds against different carcinoma cells was assayed. The results show that some compounds display a distinct antiproliferative activity against tested cancer cells and are almost inactive to HEK293T cells.
Key words: testosterone, heterosteroids, aza-A-homocholesteryl-lactam thiazole derivatives, antiproliferative activity


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