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D环取代甾体苯甲酰胺噻唑的合成及其抗增殖活性

Synthesis and antiproliferative activity of D-ring substituted steroidal benzamidothiazoles.

作者信息

Fan Ning-Juan, He Qiu-Rui, Duan Min, Bai Yu-Bin, Tang Jiang-Jiang

机构信息

Biochemistry and Molecular Biology Research Platform, College of Life Science, Northwest A&F University, Yangling, Shaanxi 712100, China.

Shaanxi Engineering Center of Bio-resource Chemistry & Sustainable Utilization, College of Science, Northwest A&F University, Yangling, Shaanxi 712100, China.

出版信息

Steroids. 2016 Aug;112:103-8. doi: 10.1016/j.steroids.2016.04.009. Epub 2016 Apr 29.

Abstract

Using progesterone as the starting material, we synthesized a series of steroidal derivatives possessing a D-ring substituted benzamidothiazole. All of the final structures were reported and identified by NMR and HRMS spectrometry for the first time. The antiproliferative activity of the synthesized compounds against PC-3 (human prostate cancer cell line) and SKOV-3 (ovarian cancer cells) were investigated. The preliminary results showed that compounds 8b, 8d and 8g possessed moderate antiproliferative activities.

摘要

以孕酮为起始原料,我们合成了一系列具有D环取代苯甲酰氨基噻唑的甾体衍生物。所有最终结构均首次通过核磁共振(NMR)和高分辨质谱(HRMS)光谱进行了报道和鉴定。研究了合成化合物对PC-3(人前列腺癌细胞系)和SKOV-3(卵巢癌细胞)的抗增殖活性。初步结果表明,化合物8b、8d和8g具有中等抗增殖活性。

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