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

doi:10.6023/cjoc201710005

Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (6): 1484-1492.DOI: 10.6023/cjoc201710005 Previous Articles Next Articles

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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

黄燕敏, 庞春玲, 杨春晖, 展军颜, 甘春芳, 庞丽萍, 刘晓兰, 崔建国

广西师范学院化学与材料科学学院南宁 530001

收稿日期:2017-10-08 修回日期:2017-12-13 发布日期:2018-02-06
通讯作者: 崔建国,E-mail:cuijg1954@126.com E-mail:cuijg1954@126.com
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

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

Received:2017-10-08 Revised:2017-12-13 Published:2018-02-06
Contact: 10.6023/cjoc201710005 E-mail:cuijg1954@126.com
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).

1. Synthesis and Evaluation of Some New Aza-A-homocholesteryl-lactam Thiazole Derivatives as Anticancer Agents.PDF(3257KB)

Abstract

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

Cite this article

Huang Yanmin, Pang Chunling, Yang Chunhui, Zhan Junyan, Gan Chunfang, Pang Liping, Liu Xiaolan, Cui Jianguo. Synthesis and Evaluation of Some New Aza-A-homocholesteryl-lactam Thiazole Derivatives as Anticancer Agents[J]. Chin. J. Org. Chem., 2018, 38(6): 1484-1492.

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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

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