Search

Your search keyword '"C. M. Camaggi"' showing total 14 results
Start Over Author "C. M. Camaggi" Topic general medicine
14 results on '"C. M. Camaggi"'

14. Design, Synthesis and Biological Evaluation of Pyrazole derivatives as Potential multikinase Inhibitors in Hepatocarcinoma

Author

Mauro Comes-Franchini, Francesca Fornari, Carlo Maurizio Camaggi, Simone Breviglieri, Manuela Minguzzi, Maddalena Milazzo, Valentina Rebuttini, Erica Locatelli, Laura Gramantieri, Luigi Bolondi, Elena Strocchi, F. Fornari, M. Minguzzi, E. Strocchi, E. Locatelli, L. Gramantieri, M. Milazzo, V. Rebuttini, S. Breviglieri, C. M. Camaggi, L. Bolondi, and M. Comes Franchini

Subjects
Models, Molecular, Spectrometry, Mass, Electrospray Ionization, Carcinoma, Hepatocellular, Magnetic Resonance Spectroscopy, Nitrile, Blotting, Western, Antineoplastic Agents, Pyrazole, Molecular Dynamics Simulation, molecular docking, kinase inhibitors, chemistry.chemical_compound, Cell Line, Tumor, Drug Discovery, medicine, Humans, Protein Kinase Inhibitors, Cell Proliferation, Pharmacology, Binding Sites, Chemistry, Kinase, Organic Chemistry, Liver Neoplasms, Biological activity, General Medicine, hepatocellular carcinoma, medicine.disease, Cycloaddition, pyrazole, Biochemistry, dipolar cycloaddition, Cell culture, Apoptosis, Hepatocellular carcinoma, Pyrazoles, Protein Kinases
Abstract

We described the optimization, by molecular modelling, of small pyrazole derivatives, as kinase inhibitors, obtained through a 1,3-dipolar cycloaddition between nitrile imines and functionalized acetylenes. The two compounds, selected as potential agents active against hepatocellular carcinoma (HCC) were then evaluated in vitro for their biological activity on HCC-derived cell lines. The compounds show a promising inhibitory growth efficacy (IC 50 50–100 μM) in SNU449 cell line, as well as block of cell cycle progression and induction of apoptosis, and can be considered as lead compounds for further SAR developments.

Published
2012

Catalog

Books, media, physical & digital resources
See catalog results