3-[4-(1H-indol-3-yl)-1,3-thiazol-2-yl]-1H-pyrrolo[2,3-b]pyridines, nortopsentin Analogues with antiproliferative activity
| Autor: | Patrizia Diana, Gloria Di Vita, Girolamo Cirrincione, M. A. Livrea, Anna Carbone, Cristina Ciancimino, Luisa Tesoriere, Paola Barraja, Alessandro Attanzio, Virginia Spanò, Barbara Parrino, Alessandra Montalbano |
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| Přispěvatelé: | Parrino, B., Carbone, A., Di Vita, G., Ciancimino, C., Attanzio, A., Spanò, V., Montalbano, A., Barraja, P., Tesoriere, L., Livrea, M., Diana, P., Cirrincione, G. |
| Jazyk: | angličtina |
| Rok vydání: | 2015 |
| Předmět: |
Indoles
Halogenation Pyridines 3-b]pyridines Pharmaceutical Science Apoptosis Antiproliferative activity 3-[4-(1H-indol-3-yl)-1 3-thiazol-2-yl]-1H-pyrrolo[2 3-b]pyridines chemistry.chemical_compound Neoplasms Drug Discovery Imidazole Moiety indolyl alkaloids Pharmacology Toxicology and Pharmaceutics (miscellaneous) lcsh:QH301-705.5 Membrane Potential Mitochondrial Molecular Structure 3-[4-(1H-indol-3-yl)-1 3-thiazol-2-yl]-1H-pyrrolo[2 Indolyl alkaloids Marine alkaloids Nortopsentin analogues Drug Discovery3003 Pharmaceutical Science Imidazoles Phosphatidylserine Mitochondria nortopsentin analogues Indolyl alkaloid marine alkaloids G2 Phase Stereochemistry Nortopsentin analogue Antineoplastic Agents Methylation Resting Phase Cell Cycle Article Alkaloids Cell Line Tumor Humans Pyrroles Thiazole Cell Proliferation Indole test Natural product Cell growth Settore CHIM/08 - Chimica Farmaceutica Thiazoles chemistry lcsh:Biology (General) Cell culture Drug Design Marine alkaloid 3-[4-(1H-indol-3-yl)-1 3-thiazol-2-yl]-1H-pyrrolo[2 3-b]pyridine |
| Zdroj: | Marine Drugs, Vol 13, Iss 4, Pp 1901-1924 (2015) Marine Drugs Volume 13 Issue 4 Pages 1901-1924 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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