title: Synthesis and structure elucidation of some novel thiophene and benzothiophene derivatives as cytotoxic agents.
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 synthesized and 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 fibro-blast human cell line (WI-38) compared to the anti-proliferative effects of the reference control doxorubicin.
authors.forename: Rafat M
authors.initials: RM
authors.lastname: Mohareb
authors.forename: Amira E M
authors.initials: AE
authors.lastname: Abdallah
authors.forename: Maher H E
authors.initials: MH
authors.lastname: Helal
authors.forename: Somiya M H
authors.initials: SM
authors.lastname: Shaloof
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002460:Cell Line; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003603:Cytotoxins / Q000138:chemical synthesis* / Q000494:pharmacology*; D004317:Doxorubicin / Q000494:pharmacology; D006801:Humans; D061986:MCF-7 Cells; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D003603:Cytotoxins; D013876:Thiophenes; C088015:benzothiophene; D004317:Doxorubicin