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

• Published in: Molecules (Basel, Switzerland) Vol. 26; no. 19; p. 5735
• Main Authors: Signorello, Maria Grazia, Rapetti, Federica, Meta, Elda, Sidibè, Adama, Bruno, Olga, Brullo, Chiara
• Format: Journal Article
• Language: English
• Published: Basel MDPI AG 22-09-2021; MDPI
• Subjects: AKT protein; Angiogenesis; Antiangiogenics; Biological activity; Blood clots; Cancer; Cytokines; Endothelial cells; imidazo-pyrazoles; Inflammation; Kinases; medicinal chemistry; Neutrophils; p38MAPK; Phosphorylation; Platelet aggregation; platelet aggregation inhibition; Pyrazoles; ROS inhibition; Thrombosis; Tumorigenesis; Umbilical vein
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules26195735

(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.