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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.
Affiliation
  • Signorello MG; Biochemistry Lab., Department of Pharmacy, University of Genoa, Viale Benedetto XV 3, I-16132 Genova, Italy.
  • Rapetti F; Section of Medicinal Chemistry, Department of Pharmacy, University of Genoa, Viale Benedetto XV 3, I-16132 Genova, Italy.
  • Meta E; Laboratory of Angiogenesis and Vascular Metabolism, Center for Cancer Biology, Vlaams Instituut Voor Biotechnologie, 3000 Leuven, Belgium.
  • Sidibè A; Department of Cell Physiology and Metabolism, University of Geneva, Rue Michel-Servet 1, CH-1211 Geneva, Switzerland.
  • Bruno O; Section of Medicinal Chemistry, Department of Pharmacy, University of Genoa, Viale Benedetto XV 3, I-16132 Genova, Italy.
  • Brullo C; Section of Medicinal Chemistry, Department of Pharmacy, University of Genoa, Viale Benedetto XV 3, I-16132 Genova, Italy.
Molecules ; 26(19)2021 Sep 22.
Article in En | MEDLINE | ID: mdl-34641279
(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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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrazoles / P38 Mitogen-Activated Protein Kinases / Small Molecule Libraries / Imidazoles / Anti-Inflammatory Agents Limits: Humans Language: En Journal: Molecules Journal subject: BIOLOGIA Year: 2021 Type: Article Affiliation country: Italy

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrazoles / P38 Mitogen-Activated Protein Kinases / Small Molecule Libraries / Imidazoles / Anti-Inflammatory Agents Limits: Humans Language: En Journal: Molecules Journal subject: BIOLOGIA Year: 2021 Type: Article Affiliation country: Italy