Citation: Cui Jianguo, Zhao Dandan, He Dongmei, Huang Yanmin, Liu Zhiping, Lin Qifu Shi, Haixin Gan, . Synthesis of Dehydroepiandrosteronyl Thiazole Derivatives and Their Antiproliferative Evaluation[J]. Chinese Journal of Organic Chemistry, ;2016, 36(3): 630-637. doi: 10.6023/cjoc201509021 shu

Synthesis of Dehydroepiandrosteronyl Thiazole Derivatives and Their Antiproliferative Evaluation

Cui Jianguo ^a,b ,
Zhao Dandan ^a ,
He Dongmei ^a ,
Huang Yanmin ^a ,
Liu Zhiping ^a ,
Lin Qifu Shi ^b ,
Haixin Gan ^b ,
^a,,

1.
a Key Laboratory of Environment Change and Resources Use in Beibu Gulf Ministry of Education, Chemistry and Materials Science College, Guangxi Teachers Education University, Nanning 530001;
2.
b Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resoure Effective Utilization, Qizhou University, Qinzhou 535000

Corresponding author: ,
Received Date: 18 September 2015
Available Online: 18 November 2015
Fund Project: 国家自然科学基金(Nos. 21462009, 21562007) (Nos. 21462009, 21562007)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) (No. 2014KLOG09)

Using dehydroepiandrosterone as starting material, 16 dehydroepiandrosteronyl thiazol derivatives with different structures had been synthesized via microwave irradiation assisted one-pot reaction and general synthetic method, and their structures were characterized by IR, NMR and HRMS. The antiproliferative activity of the compounds was evaluated against human cervical carcinoma (HeLa), human lung carcinoma (A549), human liver carcinoma cells (HEPG2) and normal kidney epithelial cells (HEK293T). The results showed that compound 4 displayed significant inhibitory activity to tested cancer cells, and the values of IC₅₀ were 13.2, 11.3 and 8.3 μmol·L^-1 respectively, but was almost inactive to HEK293T cells (IC₅₀>100 μmol·L^-1). However, other compounds did not exhibit distinct antiproliferative activity to all tested cells.
- dehydroepiandrosterone,
- thiazole,
- dehydroepiandrosteronyl thiazole derivatives,
- antiproliferative activity
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