4.6 Article

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

Journal

MOLECULES
Volume 26, Issue 19, Pages -

Publisher

MDPI
DOI: 10.3390/molecules26195735

Keywords

pyrazoles; imidazo-pyrazoles; medicinal chemistry; ROS inhibition; platelet aggregation inhibition; p38MAPK; anti-angiogenesis compounds

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By synthesizing a new small compound library, it was found that most of the newly synthesized derivatives were able to block ROS production, platelet aggregation, and p38MAPK phosphorylation, paving the way for the development of new agents with anti-angiogenic activity.
(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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