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Synthesis and Antitumor Activity of New Thiazole Nortopsentin Analogs

Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche, STEBICEF, via Archirafi 32, 90123 Palermo, Italy
Author to whom correspondence should be addressed.
Academic Editor: Orazio Taglialatela-Scafati
Mar. Drugs 2016, 14(12), 226;
Received: 10 October 2016 / Revised: 13 November 2016 / Accepted: 5 December 2016 / Published: 14 December 2016
(This article belongs to the Special Issue Synthesis of Antitumor Marine Alkaloids and Related Analogues)
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New thiazole nortopsentin analogs in which one of the two indole units was replaced by a naphthyl and/or 7-azaindolyl portion, were conveniently synthesized. Among these, three derivatives showed good antiproliferative activity, in particular against MCF7 cell line, with GI50 values in the micromolar range. Their cytotoxic effect on MCF7 cells was further investigated in order to elucidate their mode of action. Results showed that the three compounds act as pro-apoptotic agents inducing a clear shift of viable cells towards early apoptosis, while not exerting necrotic effects. They also caused cell cycle perturbation with significant decrease in the percentage of cells in the G0/G1 and S phases, accompanied by a concomitant percentage increase of cells in the G2/M phase, and appearance of a subG1-cell population. View Full-Text
Keywords: marine alkaloids; bis-indolyl alkaloids; thiazolyl-indoles; apoptosis; antiproliferative activity marine alkaloids; bis-indolyl alkaloids; thiazolyl-indoles; apoptosis; antiproliferative activity

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Spanò, V.; Attanzio, A.; Cascioferro, S.; Carbone, A.; Montalbano, A.; Barraja, P.; Tesoriere, L.; Cirrincione, G.; Diana, P.; Parrino, B. Synthesis and Antitumor Activity of New Thiazole Nortopsentin Analogs. Mar. Drugs 2016, 14, 226.

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