Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity

Twenty-four new hybrid analogues (15–38) containing 7-chloro-4-aminoquinoline and 2-pyrazoline N-heterocyclic fragments were synthesized. Twelve of the new compounds were evaluated against 58 human cancer cell lines by the U.S. National Cancer Institute (NCI). Compounds 25, 30, 31, 36, and 37 showed...

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Autores principales: Montoya, Alba, Quiroga, Jairo, Abonia, Rodrigo, Derita, Marcos, Sortino, Maximiliano, Ornelas, Alfredo, Zacchino, Susana, Insuasty, Braulio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6274157/
https://www.ncbi.nlm.nih.gov/pubmed/27472314
http://dx.doi.org/10.3390/molecules21080969
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author Montoya, Alba
Quiroga, Jairo
Abonia, Rodrigo
Derita, Marcos
Sortino, Maximiliano
Ornelas, Alfredo
Zacchino, Susana
Insuasty, Braulio
author_facet Montoya, Alba
Quiroga, Jairo
Abonia, Rodrigo
Derita, Marcos
Sortino, Maximiliano
Ornelas, Alfredo
Zacchino, Susana
Insuasty, Braulio
author_sort Montoya, Alba
collection PubMed
description Twenty-four new hybrid analogues (15–38) containing 7-chloro-4-aminoquinoline and 2-pyrazoline N-heterocyclic fragments were synthesized. Twelve of the new compounds were evaluated against 58 human cancer cell lines by the U.S. National Cancer Institute (NCI). Compounds 25, 30, 31, 36, and 37 showed significant cytostatic activity, with the most outstanding GI(50) values ranging from 0.05 to 0.95 µM. The hybrid compounds (15–38) were also evaluated for antifungal activity against Candida albicans and Cryptococcus neoformans. From the obtained results some structure–activity relationships were outlined.
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spelling pubmed-62741572018-12-28 Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity Montoya, Alba Quiroga, Jairo Abonia, Rodrigo Derita, Marcos Sortino, Maximiliano Ornelas, Alfredo Zacchino, Susana Insuasty, Braulio Molecules Article Twenty-four new hybrid analogues (15–38) containing 7-chloro-4-aminoquinoline and 2-pyrazoline N-heterocyclic fragments were synthesized. Twelve of the new compounds were evaluated against 58 human cancer cell lines by the U.S. National Cancer Institute (NCI). Compounds 25, 30, 31, 36, and 37 showed significant cytostatic activity, with the most outstanding GI(50) values ranging from 0.05 to 0.95 µM. The hybrid compounds (15–38) were also evaluated for antifungal activity against Candida albicans and Cryptococcus neoformans. From the obtained results some structure–activity relationships were outlined. MDPI 2016-07-27 /pmc/articles/PMC6274157/ /pubmed/27472314 http://dx.doi.org/10.3390/molecules21080969 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Montoya, Alba
Quiroga, Jairo
Abonia, Rodrigo
Derita, Marcos
Sortino, Maximiliano
Ornelas, Alfredo
Zacchino, Susana
Insuasty, Braulio
Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity
title Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity
title_full Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity
title_fullStr Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity
title_full_unstemmed Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity
title_short Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity
title_sort hybrid molecules containing a 7-chloro-4-aminoquinoline nucleus and a substituted 2-pyrazoline with antiproliferative and antifungal activity
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6274157/
https://www.ncbi.nlm.nih.gov/pubmed/27472314
http://dx.doi.org/10.3390/molecules21080969
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