Acta Pharmaceutica, Vol. 66 No. 1, 2016.
Original scientific paper
https://doi.org/10.1515/acph-2016-0005
Synthesis and structure elucidation of some novel thiophene and benzothiophene derivatives as cytotoxic agents
RAFAT M. MOHAREB
; Department of Chemistry, Faculty of Science, Cairo University, Giza, A. R. Egypt
AMIRA. E. M. ABDALLAH
; Department of Chemistry, Faculty of Science, Helwan University, AinHelwan, Cairo A. R. Egypt
MAHER H. E. HELAL
; Department of Chemistry, Faculty of Science, Helwan University, AinHelwan, Cairo A. R. Egypt
SOMIYA M. H. SHALOOF
; Department of Chemistry, Faculty of Science, Western MountainUniversity, Alzintan, Libya
Abstract
Attempting to produce cyclized systems with potential anti-proliferative activity, a series of novel thiophene and benzothiophene derivatives were designed and synthesized. The reactivity of the latter derivatives towards different chemical reagents was studied. Twenty-one compounds were evaluated as anti-cancer agents. The results showed that ethyl 5-amino-3-(4-chlorostyryl)-4-cyanothiophene-2-carboxylate (5b) ethyl 5-amino-4-((4-methoxyphenyl)carbonyl)-3-methylhiophene-2-carboxylate (8c) and 5-3-(ethoxy-3-oxopropanamido)-3-methyl-4-(phenylcarbamoyl)thiophene-2-carboxylate (9) were the most active compounds towards three tumor cell lines – MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) and SF-268 (CNS cancer) and a normal fibroblast human cell line (WI-38), compared to the anti-proliferative effects of the reference control doxorubicin.
Keywords
thiophene; benzothiophene; cytotoxic agents
Hrčak ID:
146014
URI
Publication date:
31.3.2016.
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