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脱氢表雄酮稠合噻唑、咪唑并[2,1 - b]噻唑、吡啶甾体类似物的合成及生物学评价

Synthesis and biological evaluation of dehydroepiandrosterone-fused thiazole, imidazo[2,1-b]thiazole, pyridine steroidal analogues.

作者信息

Zhang Bao-Le, Song Li-Xing, Li Ya-Fei, Li Yi-Lei, Guo Ya-Zhuo, Zhang En, Liu Hong-Min

机构信息

School of Pharmaceutical Sciences and New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, PR China.

School of Pharmaceutical Sciences and New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, PR China.

出版信息

Steroids. 2014 Feb;80:92-101. doi: 10.1016/j.steroids.2013.12.003. Epub 2013 Dec 16.

DOI:10.1016/j.steroids.2013.12.003
PMID:24355392
Abstract

A series of steroidal[17,16-d]thiazole, steroidal[1,2-b]pyridine and steroidal[17,16-d]thiazole[2,1-b]imidazo products were synthesized through a convenient and productive method. Anti-proliferation activity against EC109 (human esophageal carcinoma), EC9706 (human esophageal carcinoma) and MGC-803 (human gastric carcinoma) cell lines was examined in vitro. Among the screened compounds, several highly potential compounds were located.

摘要

通过一种简便高效的方法合成了一系列甾体[17,16 - d]噻唑、甾体[1,2 - b]吡啶和甾体[17,16 - d]噻唑[2,1 - b]咪唑产物。体外检测了它们对EC109（人食管癌）、EC9706（人食管癌）和MGC - 803（人胃癌）细胞系的抗增殖活性。在筛选出的化合物中，找到了几种极具潜力的化合物。

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