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
收稿日期: 2017-10-08
修回日期: 2017-12-13
网络出版日期: 2018-02-06
基金资助
国家自然科学基金（Nos.21462009，21562007）、南宁市科技开发项目（No.20171125-5）和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.
Synthesis and Evaluation of Some New Aza-A-homocholesteryl-lactam Thiazole Derivatives as Anticancer Agents
Received date: 2017-10-08
Revised date: 2017-12-13
Online published: 2018-02-06
Supported by
Project supported by the National Natural Science Foundation of China (Nos. 21462009, 21562007), the Technology and Development Project of Nanning City (No. 20171125-5), the Guangxi Colleges and University Key Laboratory Foundation of Beibu Gulf Oil and Natural Gas Resource Effective Utilization (No. 2014KLOG09).
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
黄燕敏 , 庞春玲 , 杨春晖 , 展军颜 , 甘春芳 , 庞丽萍 , 刘晓兰 , 崔建国 . 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[J]. 有机化学, 2018 , 38(6) : 1484 -1492 . DOI: 10.6023/cjoc201710005
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.
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