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New Series of Pyrazoles and Imidazo-Pyrazoles Targeting Different Cancer and Inflammation Pathways

(1) Background: different previously synthesized pyrazoles and imidazo-pyrazoles showed interesting anti-angiogenic action, being able to interfere with ERK1/2, AKT and p38MAPK phosphorylation in different manners and with different potency; (2) Methods: here, a new small compound library, endowed w...

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Autores principales: Signorello, Maria Grazia, Rapetti, Federica, Meta, Elda, Sidibè, Adama, Bruno, Olga, Brullo, Chiara
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8510017/
https://www.ncbi.nlm.nih.gov/pubmed/34641279
http://dx.doi.org/10.3390/molecules26195735
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author Signorello, Maria Grazia
Rapetti, Federica
Meta, Elda
Sidibè, Adama
Bruno, Olga
Brullo, Chiara
author_facet Signorello, Maria Grazia
Rapetti, Federica
Meta, Elda
Sidibè, Adama
Bruno, Olga
Brullo, Chiara
author_sort Signorello, Maria Grazia
collection PubMed
description (1) Background: different previously synthesized pyrazoles and imidazo-pyrazoles showed interesting anti-angiogenic action, being able to interfere with ERK1/2, AKT and p38MAPK phosphorylation in different manners and with different potency; (2) Methods: here, a new small compound library, endowed with the same differently decorated chemical scaffolds, has been synthetized to obtain new agents able to inhibit different pathways involved in inflammation, cancer and human platelet aggregation. (3) Results: most of the new synthesized derivatives resulted able to block ROS production, platelet aggregation and p38MAPK phosphorylation both in platelets and Human Umbilical Vein Endothelial cells (HUVEC). This paves the way for the development of new agents with anti-angiogenic activity.
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spelling pubmed-85100172021-10-13 New Series of Pyrazoles and Imidazo-Pyrazoles Targeting Different Cancer and Inflammation Pathways Signorello, Maria Grazia Rapetti, Federica Meta, Elda Sidibè, Adama Bruno, Olga Brullo, Chiara Molecules Article (1) Background: different previously synthesized pyrazoles and imidazo-pyrazoles showed interesting anti-angiogenic action, being able to interfere with ERK1/2, AKT and p38MAPK phosphorylation in different manners and with different potency; (2) Methods: here, a new small compound library, endowed with the same differently decorated chemical scaffolds, has been synthetized to obtain new agents able to inhibit different pathways involved in inflammation, cancer and human platelet aggregation. (3) Results: most of the new synthesized derivatives resulted able to block ROS production, platelet aggregation and p38MAPK phosphorylation both in platelets and Human Umbilical Vein Endothelial cells (HUVEC). This paves the way for the development of new agents with anti-angiogenic activity. MDPI 2021-09-22 /pmc/articles/PMC8510017/ /pubmed/34641279 http://dx.doi.org/10.3390/molecules26195735 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Signorello, Maria Grazia
Rapetti, Federica
Meta, Elda
Sidibè, Adama
Bruno, Olga
Brullo, Chiara
New Series of Pyrazoles and Imidazo-Pyrazoles Targeting Different Cancer and Inflammation Pathways
title New Series of Pyrazoles and Imidazo-Pyrazoles Targeting Different Cancer and Inflammation Pathways
title_full New Series of Pyrazoles and Imidazo-Pyrazoles Targeting Different Cancer and Inflammation Pathways
title_fullStr New Series of Pyrazoles and Imidazo-Pyrazoles Targeting Different Cancer and Inflammation Pathways
title_full_unstemmed New Series of Pyrazoles and Imidazo-Pyrazoles Targeting Different Cancer and Inflammation Pathways
title_short New Series of Pyrazoles and Imidazo-Pyrazoles Targeting Different Cancer and Inflammation Pathways
title_sort new series of pyrazoles and imidazo-pyrazoles targeting different cancer and inflammation pathways
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8510017/
https://www.ncbi.nlm.nih.gov/pubmed/34641279
http://dx.doi.org/10.3390/molecules26195735
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