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EnglishA series of substituted ethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5- (1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)carbonyl]-1H-pyrrole-3-carboxylates were prepared in excellent yields (82-98%) by one-pot reactions between β-dicarbonyl compounds 12a–e and 1,2-diaza-1,3-diene (DD) 13. Derivatives 10a,c–e, deazaanalogues of the bis-indole alkaloid topsentin, screened by the National Cancer Institute (Bethesda, MD, USA) in the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity, with the exception of compound 9e, which showed moderate activity against the HOP-92 cell line of the non small cell lung cancer sub-panel and the SNB-75 cell line of the CNS sub-panel.
| Data di pubblicazione: | 2013 |
| Titolo: | A Facile Synthesis of Deaza-Analogues of the Bisindole Marine Alkaloid Topsentin |
| Autori: | |
| Citazione: | Carbone, A., Spano', V., Parrino, B., Ciancimino, C., Attanasi, O., & Favi, G. (2013). A Facile Synthesis of Deaza-Analogues of the Bisindole Marine Alkaloid Topsentin. MOLECULES, 18, 2518-2527. |
| Rivista: | |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.3390/molecules18032518 |
| Abstract: | A series of substituted ethyl 1-[(tert-butoxycarbonyl)amino]-2-methyl-5- (1-methyl-1H-indol-3-yl)-4-[(1-methyl-1H-indol-3-yl)carbonyl]-1H-pyrrole-3-carboxylates were prepared in excellent yields (82-98%) by one-pot reactions between β-dicarbonyl compounds 12a–e and 1,2-diaza-1,3-diene (DD) 13. Derivatives 10a,c–e, deazaanalogues of the bis-indole alkaloid topsentin, screened by the National Cancer Institute (Bethesda, MD, USA) in the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity, with the exception of compound 9e, which showed moderate activity against the HOP-92 cell line of the non small cell lung cancer sub-panel and the SNB-75 cell line of the CNS sub-panel. |
| Settore Scientifico Disciplinare: | Settore CHIM/08 - Chimica Farmaceutica |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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