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标题：Synthesis and cytotoxicity evaluation of thiazole derivatives obtained from 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene3-carbonitrile
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作者：RAFAT M. MOHAREB ; AMIRA E. M. ABDALLAH ; EBTSAM A. AHMED 等
期刊名称：Acta Pharmaceutica
电子版ISSN：1846-9558
出版年度：2017
卷号：67
期号：4
页码：495-510
DOI：10.1515//acph-2017-0040
语种：English
出版社：Sciendo
摘要：Reactivity of 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene3-carbonitrile towards thioglycolic acid resulted in thiazole derivative 1.The latter reacted with different chemical reagents to give thiazole,pyrano[2,3-d]thiazole and thiazolo[4,5-d]thiazole derivatives.Cytotoxicity effects of the newly synthesized products against six cancer cell lines,namely,human gastric cancer (NUGC),human colon cancer (DLD1),human liver cancer (HA22T and HEPG-2),human breast cancer (MCF) and nasopharyngeal carcinoma (HONE-1) as well as against a normal fibroblast cell (WI-38) were evaluated.The study showed that the 4,5,6,7 tetrahydrobenzo[b] thiophene derivatives 6a,7,8a,b,9b and 10b,c were the most active compounds.Their potencies were attributed to the presence of the electron withdrawing groups.
关键词：tetrahydrobenzo[b]thiophene;thiazole;pyrano[2;3-d]thiazole;thiazolo[4;5-d]thiazole;cytotoxicity;anticancer activity