期刊
ACTA PHARMACEUTICA
卷 67, 期 4, 页码 495-510出版社
HRVATSKO FARMACEUTSKO DRUSTOV (HFD)-CROATION PHARMACEUTICAL SOC
DOI: 10.1515/acph-2017-0040
关键词
tetrahydrobenzo[b]thiophene; thiazole; pyrano[2,3-d]thiazole; thiazolo[4,5-d]thiazole; cytotoxicity; anti-cancer activity
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.
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