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EnglishA new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (∼60) having GI50 values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunction. Moreover, the compounds induced a concentration-dependent accumulation of cells in the subG0/G1phase, while confined viable cells in G2/M phase.
Parrino, B., Carbone, A., Di Vita, G., Ciancimino, C., Attanzio, A., Spanò, V., et al. (2015). 3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin Analogues with antiproliferative activity. MARINE DRUGS, 13(4), 1901-1924.
| Data di pubblicazione: | 2015 |
| Titolo: | 3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin Analogues with antiproliferative activity |
| Autori: | |
| Citazione: | Parrino, B., Carbone, A., Di Vita, G., Ciancimino, C., Attanzio, A., Spanò, V., et al. (2015). 3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin Analogues with antiproliferative activity. MARINE DRUGS, 13(4), 1901-1924. |
| Rivista: | |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.3390/md13041901 |
| Abstract: | A new series of nortopsentin analogues, in which the imidazole ring of the natural product was replaced by thiazole and the indole unit bound to position 2 of the thiazole ring was substituted by a 7-azaindole moiety, was efficiently synthesized. Two of the new nortopsentin analogues showed good antiproliferative effect against the totality of the NCI full panel of human tumor cell lines (∼60) having GI50 values ranging from low micromolar to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, investigated on human hepatoma HepG2 cells, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and mitochondrial dysfunction. Moreover, the compounds induced a concentration-dependent accumulation of cells in the subG0/G1phase, while confined viable cells in G2/M phase. |
| URL: | http://www.mdpi.com/1660-3397/13/4/1901/pdf |
| Settore Scientifico Disciplinare: | Settore CHIM/08 - Chimica Farmaceutica |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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| File | Descrizione | Tipologia | Licenza | |
|---|---|---|---|---|
| Marine Drugs 13, 1901-1924, 2015.pdf | articolo principale | Versione Editoriale | Open Access Visualizza/Apri |
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