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.

Spanò, V., Attanzio, A., Cascioferro, S., Carbone, A., Montalbano, A., Barraja, P., et al. (2016). Synthesis and antitumor activity of new thiazole nortopsentin analogs. MARINE DRUGS, 14(12), 1-18 [10.3390/md14120226].

Synthesis and antitumor activity of new thiazole nortopsentin analogs

SPANO', Virginia;ATTANZIO, Alessandro;CASCIOFERRO, Stella Maria;CARBONE, Anna;MONTALBANO, Alessandra;BARRAJA, Paola;TESORIERE, Luisa;CIRRINCIONE, Girolamo;DIANA, Patrizia;PARRINO, Barbara
2016-12-14

Abstract

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.
Settore CHIM/08 - Chimica Farmaceutica
https://www.mdpi.com/1660-3397/14/12/226
https://www.scopus.com/sourceid/144790?origin=recordpage
Spanò, V., Attanzio, A., Cascioferro, S., Carbone, A., Montalbano, A., Barraja, P., et al. (2016). Synthesis and antitumor activity of new thiazole nortopsentin analogs. MARINE DRUGS, 14(12), 1-18 [10.3390/md14120226].
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/10447/222770
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