Cargando…
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...
Autores principales: | , , , , , |
---|---|
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 |
_version_ | 1784582474328702976 |
---|---|
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. |
format | Online Article Text |
id | pubmed-8510017 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT signorellomariagrazia newseriesofpyrazolesandimidazopyrazolestargetingdifferentcancerandinflammationpathways AT rapettifederica newseriesofpyrazolesandimidazopyrazolestargetingdifferentcancerandinflammationpathways AT metaelda newseriesofpyrazolesandimidazopyrazolestargetingdifferentcancerandinflammationpathways AT sidibeadama newseriesofpyrazolesandimidazopyrazolestargetingdifferentcancerandinflammationpathways AT brunoolga newseriesofpyrazolesandimidazopyrazolestargetingdifferentcancerandinflammationpathways AT brullochiara newseriesofpyrazolesandimidazopyrazolestargetingdifferentcancerandinflammationpathways |