Synthesis and Antitumor Activity of New Thiazole Nortopsentin Analogs

Marine Drugs

Barbara Parrino¹  Virginia Spanò¹  Alessandro Attanzio¹  Anna Carbone¹  Stella Cascioferro¹  Luisa Tesoriere¹  Paola Barraja¹  Alessandra Montalbano¹  Girolamo Cirrincione¹  Patrizia Diana¹ 

[1] Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche, STEBICEF, via Archirafi 32, 90123 Palermo, Italy;

关键词: marine alkaloids;    bis-indolyl alkaloids;    thiazolyl-indoles;    apoptosis;    antiproliferative activity;   

DOI  :  10.3390/md14120226

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown