Rapid Microwave Assisted Synthesis and Antiproliferative Evaluation of Novel Steroidal Thiazole Derivatives

doi:10.1007/s40242-017-6372-y

高等学校化学研究 ›› 2017, Vol. 33 ›› Issue (2): 206-212.doi: 10.1007/s40242-017-6372-y

Rapid Microwave Assisted Synthesis and Antiproliferative Evaluation of Novel Steroidal Thiazole Derivatives

HUANG Yanmin¹, ZHAO Dandan¹, LIU Chang¹, GAN Chunfang¹, ZHAN Junyan¹, LIN Qifu², SHI Haixin², CUI Jianguo^1,2

1. College of Chemistry and Material Science, Guangxi Teachers Education University, Nanning 530001, P. R. China;
2. Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resource Effective Utilization, Qizhou University, Qizhou 535011, P. R. China

收稿日期:2016-09-05 修回日期:2016-09-18 出版日期:2017-04-01 发布日期:2017-03-23
通讯作者: CUI Jianguo,E-mail:cuijg1954@126.com E-mail:cuijg1954@126.com
基金资助:
Supported by the National Natural Science Foundation of China(Nos.21462009, 21562007) and the Foundation of Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resource Effective Utilization, China(No. 2016kLOG10).

Rapid Microwave Assisted Synthesis and Antiproliferative Evaluation of Novel Steroidal Thiazole Derivatives

HUANG Yanmin¹, ZHAO Dandan¹, LIU Chang¹, GAN Chunfang¹, ZHAN Junyan¹, LIN Qifu², SHI Haixin², CUI Jianguo^1,2

1. College of Chemistry and Material Science, Guangxi Teachers Education University, Nanning 530001, P. R. China;
2. Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resource Effective Utilization, Qizhou University, Qizhou 535011, P. R. China

Received:2016-09-05 Revised:2016-09-18 Online:2017-04-01 Published:2017-03-23
Contact: CUI Jianguo,E-mail:cuijg1954@126.com E-mail:cuijg1954@126.com
Supported by:
Supported by the National Natural Science Foundation of China(Nos.21462009, 21562007) and the Foundation of Guangxi Colleges and University Key Laboratory of Beibu Gulf Oil and Natural Gas Resource Effective Utilization, China(No. 2016kLOG10).

摘要/Abstract

摘要：

Three series of novel steroidal thiazole derivatives were synthesized by microwave assisted one-pot reaction from pregnenolone, testosterone and estrone, respectively. Their structures were characterized by IR, NMR and HRMS, and the antiproliferative activities of all the synthesized compounds against human cervical carcinoma (HeLa), human liver carcinoma(HepG2), human lung carcinoma(A549), nasopharyngeal carcinoma(CNE2) and normal kidney epithelial cells(HEK293T) were screened. Among the compounds, 1-estron-17'-ylidene-2-[4'-(p-bromophenyl)-2'-thiazol]hydrazone(12) displayed distinct antiproliferative activity against all the tested cancer cell lines and was almost inactive to normal kidney epithelial cells.

关键词: Microwave assisted synthesis, Pregnenolone, Testosterone, Estrone, Steroidal thiazole derivative

Abstract:

Key words: Microwave assisted synthesis, Pregnenolone, Testosterone, Estrone, Steroidal thiazole derivative

HUANG Yanmin, ZHAO Dandan, LIU Chang, GAN Chunfang, ZHAN Junyan, LIN Qifu, SHI Haixin, CUI Jianguo. Rapid Microwave Assisted Synthesis and Antiproliferative Evaluation of Novel Steroidal Thiazole Derivatives[J]. 高等学校化学研究, 2017, 33(2): 206-212.

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Rapid Microwave Assisted Synthesis and Antiproliferative Evaluation of Novel Steroidal Thiazole Derivatives

Rapid Microwave Assisted Synthesis and Antiproliferative Evaluation of Novel Steroidal Thiazole Derivatives

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