某些A-homo甾体内酰胺噻唑衍生物的合成及抗肿瘤活性评估  

Synthesis and Evaluation of Some New Aza-A-homocholesteryl-lactam Thiazole Derivatives as Anticancer Agents

作　　者：黄燕敏 庞春玲 杨春晖 展军颜 甘春芳 庞丽萍 刘晓兰 崔建国 Huang Yanmin;Pang Chunling;Yang Chunhui;Zhan Junyan;Gan Chunfang;Pang Liping;Liu Xiaolan;Cui Jianguo(College of Chemistry and Material Science, Guangxi Teachers Education University, Nanning 530001)

机构地区：[1]广西师范学院化学与材料科学学院,南宁530001

出　　处：《有机化学》2018年第6期1484-1492,共9页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(Nos.21462009;21562007);南宁市科技开发项目(No.20171125-5);广西高校北部湾石油天然气资源有效利用重点实验室开放课题(No.2014KLOG09)资助项目~~

摘　　要：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.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 var- ious heterocycles, and their structures were determined by IR, NMR and HRMS. The antiproliferative activity of the com- pounds against different carcinoma cells was assayed. The results show that some compounds display a distinct antiprolifera- tive activity against tested cancer cells and are almost inactive to HEK293T cells.

关 键 词：睾酮 甾体杂环化合物 A.Homo甾体内酰胺噻哗衍生物 抗肿瘤活性 

分 类 号：O626[理学—有机化学] TQ460.1[理学—化学]