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

descriptionPublicationkeyboard_double_arrow_right Article , Other literature type 22 Sep 2021 Italy Publisher:MDPI AGJournal:Molecules, volume 26, page 5,735 (eissn: 1420-3049,

Authors: Signorello M. G.; Rapetti F.; Meta E.; Sidibe A.; Bruno O.; Brullo C.;

doi: 10.3390/molecules26195735

pmid: 34641279

pmc: PMC8510017

handle: 11567/1062564

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

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Abstract

(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.

Country

Italy

Related Organizations

University of Geneva
Switzerland
University of Genoa
Italy
Vlaams Instituut voor Biotechnologie
Belgium
Goa University
India

Keywords

imidazo-pyrazoles, Platelet Aggregation, Anti-Inflammatory Agents, Organic chemistry, p38 Mitogen-Activated Protein Kinases, Article, Small Molecule Libraries, Structure-Activity Relationship, anti-angiogenesis compounds, QD241-441, medicinal chemistry, ROS inhibition, Human Umbilical Vein Endothelial Cells, Humans, Phosphorylation, Imidazoles, pyrazoles, platelet aggregation inhibition, Anti‐angiogenesis compounds; Imidazo‐pyrazoles; Medicinal chemistry; P38MAPK; Platelet aggregation inhibition; Pyrazoles; ROS inhibition, p38MAPK, Pyrazoles, Reactive Oxygen Species

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	citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).	9
	popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.	Top 10%
	influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).	Average
	impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.	Top 10%