Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin

2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards a panel of 42 human tumor cell lines with mean IC(50) value...

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Autores principales: Carbone, Anna, Parrino, Barbara, Barraja, Paola, Spanò, Virginia, Cirrincione, Girolamo, Diana, Patrizia, Maier, Armin, Kelter, Gerhard, Fiebig, Heinz-Herbert
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3705363/
https://www.ncbi.nlm.nih.gov/pubmed/23455514
http://dx.doi.org/10.3390/md11030643
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author Carbone, Anna
Parrino, Barbara
Barraja, Paola
Spanò, Virginia
Cirrincione, Girolamo
Diana, Patrizia
Maier, Armin
Kelter, Gerhard
Fiebig, Heinz-Herbert
author_facet Carbone, Anna
Parrino, Barbara
Barraja, Paola
Spanò, Virginia
Cirrincione, Girolamo
Diana, Patrizia
Maier, Armin
Kelter, Gerhard
Fiebig, Heinz-Herbert
author_sort Carbone, Anna
collection PubMed
description 2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards a panel of 42 human tumor cell lines with mean IC(50) values of 1.54 μM and 0.67 μM, respectively. Investigating human tumor xenografts in an ex-vivo clonogenic assay revealed selective antitumor activity, whereas sensitive tumor models were scattered among various tumor histotypes.
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spelling pubmed-37053632013-07-09 Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin Carbone, Anna Parrino, Barbara Barraja, Paola Spanò, Virginia Cirrincione, Girolamo Diana, Patrizia Maier, Armin Kelter, Gerhard Fiebig, Heinz-Herbert Mar Drugs Article 2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards a panel of 42 human tumor cell lines with mean IC(50) values of 1.54 μM and 0.67 μM, respectively. Investigating human tumor xenografts in an ex-vivo clonogenic assay revealed selective antitumor activity, whereas sensitive tumor models were scattered among various tumor histotypes. MDPI 2013-03-01 /pmc/articles/PMC3705363/ /pubmed/23455514 http://dx.doi.org/10.3390/md11030643 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Carbone, Anna
Parrino, Barbara
Barraja, Paola
Spanò, Virginia
Cirrincione, Girolamo
Diana, Patrizia
Maier, Armin
Kelter, Gerhard
Fiebig, Heinz-Herbert
Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin
title Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin
title_full Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin
title_fullStr Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin
title_full_unstemmed Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin
title_short Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin
title_sort synthesis and antiproliferative activity of 2,5-bis(3′-indolyl)pyrroles, analogues of the marine alkaloid nortopsentin
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3705363/
https://www.ncbi.nlm.nih.gov/pubmed/23455514
http://dx.doi.org/10.3390/md11030643
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