Potent and Selective Aurora Inhibitors Identified by the Expansion of a Novel Scaffold for Protein Kinase Inhibition
Journal of Medicinal Chemistry2005Vol. 48(8), pp. 3080–3084
Citations Over TimeTop 10% of 2005 papers
Daniele Fancelli, Daniela Berta, Simona Bindi, Alexander D. Cameron, Paolo Cappella, Patrizia Carpinelli, Cornel Catana, Barbara Forte, Patrizia Giordano, Maria Laura Giorgini, Sergio Mantegani, Aurelio Marsiglio, Maurizio Meroni, Juergen Moll, Valeria Pittalà, Fulvia Roletto, D. Severino, Chiara Soncini, Paola Storici, R. Tonani, Mario Varasi, Anna Vulpetti, Paola Vianello
Abstract
Potent and selective Aurora kinase inhibitors were identified from the combinatorial expansion of the 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole bi-cycle, a novel and versatile scaffold designed to target the ATP pocket of protein kinases. The most potent compound reported in this study had an IC(50) of 0.027 microM in the enzymatic assay for Aur-A inhibition and IC(50)s between 0.05 microM and 0.5 microM for the inhibition of proliferation of different tumor cell lines.
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