Synthesis and cytotoxicity evaluation of thiazole derivatives obtained from 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile

被引：25

作者：

Mohareb, Rafat M. ^{[1
]}

Abdallah, Amira E. M. ^{[2
]}

Ahmed, Ebtsam A. ^{[2
]}

机构：

[1] Cairo Univ, Fac Sci, Dept Chem, Giza, Egypt

[2] Helwan Univ Ain Helwan, Fac Sci, Dept Chem, Cairo, Egypt

来源：

ACTA PHARMACEUTICA | 2017年 / 67卷 / 04期

关键词：

tetrahydrobenzo[b]thiophene; thiazole; pyrano[2,3-d]thiazole; thiazolo[4,5-d]thiazole; cytotoxicity; anti-cancer activity; ANTIMICROBIAL ACTIVITY; HYDRAZONE; OXAZOLE;

D O I：

10.1515/acph-2017-0040

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Reactivity of 2-amino-4,5,6,7-tetrahydrobenzo[b] thiophene-3-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 thia-zo-lo[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 tetra-hy-dro-benzo[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.

引用

页码：495 / 510

页数：16

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