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Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents

A new series of 1,3,5-triazine-containing 2-pyrazoline derivatives (8–11)a–g was synthesized by cyclocondensation reactions of [(4,6-bis((2-hydroxyethyl)amino)-1,3,5-triazin-2-yl)amine]chalcones 7a–g with hydrazine hydrate and derivatives. Chalcones 7a–g were obtained by Claisen-Schmidt condensation...

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Detalles Bibliográficos
Autores principales: Moreno, Leydi M., Quiroga, Jairo, Abonia, Rodrigo, Ramírez-Prada, Jonathan, Insuasty, Braulio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6222643/
https://www.ncbi.nlm.nih.gov/pubmed/30082588
http://dx.doi.org/10.3390/molecules23081956
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author Moreno, Leydi M.
Quiroga, Jairo
Abonia, Rodrigo
Ramírez-Prada, Jonathan
Insuasty, Braulio
author_facet Moreno, Leydi M.
Quiroga, Jairo
Abonia, Rodrigo
Ramírez-Prada, Jonathan
Insuasty, Braulio
author_sort Moreno, Leydi M.
collection PubMed
description A new series of 1,3,5-triazine-containing 2-pyrazoline derivatives (8–11)a–g was synthesized by cyclocondensation reactions of [(4,6-bis((2-hydroxyethyl)amino)-1,3,5-triazin-2-yl)amine]chalcones 7a–g with hydrazine hydrate and derivatives. Chalcones 7a–g were obtained by Claisen-Schmidt condensation between aromatic aldehydes and triazinic derivative 5, which was synthesized in high yield by a microwave-assisted reaction. Seventeen of the synthesized compounds were selected and tested by the US National Cancer Institute (NCI) for their anticancer activity against 58 different human tumor cell lines. Compounds 7g and 10d,e,g showed important GI(50) values ranging from 0.569 to 16.6 µM and LC(50) values ranging from 5.15 to >100 µM.
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spelling pubmed-62226432018-11-13 Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents Moreno, Leydi M. Quiroga, Jairo Abonia, Rodrigo Ramírez-Prada, Jonathan Insuasty, Braulio Molecules Article A new series of 1,3,5-triazine-containing 2-pyrazoline derivatives (8–11)a–g was synthesized by cyclocondensation reactions of [(4,6-bis((2-hydroxyethyl)amino)-1,3,5-triazin-2-yl)amine]chalcones 7a–g with hydrazine hydrate and derivatives. Chalcones 7a–g were obtained by Claisen-Schmidt condensation between aromatic aldehydes and triazinic derivative 5, which was synthesized in high yield by a microwave-assisted reaction. Seventeen of the synthesized compounds were selected and tested by the US National Cancer Institute (NCI) for their anticancer activity against 58 different human tumor cell lines. Compounds 7g and 10d,e,g showed important GI(50) values ranging from 0.569 to 16.6 µM and LC(50) values ranging from 5.15 to >100 µM. MDPI 2018-08-06 /pmc/articles/PMC6222643/ /pubmed/30082588 http://dx.doi.org/10.3390/molecules23081956 Text en © 2018 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
Moreno, Leydi M.
Quiroga, Jairo
Abonia, Rodrigo
Ramírez-Prada, Jonathan
Insuasty, Braulio
Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents
title Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents
title_full Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents
title_fullStr Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents
title_full_unstemmed Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents
title_short Synthesis of New 1,3,5-Triazine-Based 2-Pyrazolines as Potential Anticancer Agents
title_sort synthesis of new 1,3,5-triazine-based 2-pyrazolines as potential anticancer agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6222643/
https://www.ncbi.nlm.nih.gov/pubmed/30082588
http://dx.doi.org/10.3390/molecules23081956
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