Molecules 2020 Apr 7;25(7). Epub 2020 Apr 7.
Dipartimento di Scienze della Vita e Biotecnologie, Università di Ferrara, 44121 Ferrara, Italy.
Two novel series of compounds based on the 4,5,6,7-tetrahydrothieno[2,3-]pyridine and 4,5,6,7-tetrahydrobenzothiophene molecular skeleton, characterized by the presence of a 3',4',5'-trimethoxyanilino moiety and a cyano or an alkoxycarbonyl group at its 2- or 3-position, respectively, were designed, synthesized, and evaluated for antiproliferative activity on a panel of cancer cell lines and for selected highly active compounds, inhibition of tubulin polymerization, and cell cycle effects. We have identified the 2-(3',4',5'-trimethoxyanilino)-3-cyano-6-methoxycarbonyl-4,5,6,7-tetrahydrothieno[2,3-]pyridine derivative and its 6-ethoxycarbonyl homologue as new antiproliferative agents that inhibit cancer cell growth with IC values ranging from 1.1 to 4. Read More