Potent and selective aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition

Daniele Fancelli, Daniela Berta, Simona Bindi, Alexander 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, Dino Severino, Chiara Soncini, Paola Storici, Roberto TonaniMario Varasi, Anna Vulpetti, Paola Vianello

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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 μM in the enzymatic assay for Aur-A inhibition and IC50s between 0.05 μM and 0.5 μM for the inhibition of proliferation of different tumor cell lines.

Original languageEnglish
Pages (from-to)3080-3084
Number of pages5
JournalJournal of Medicinal Chemistry
Volume48
Issue number8
DOIs
Publication statusPublished - Apr 21 2005

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ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Fancelli, D., Berta, D., Bindi, S., Cameron, A., Cappella, P., Carpinelli, P., Catana, C., Forte, B., Giordano, P., Giorgini, M. L., Mantegani, S., Marsiglio, A., Meroni, M., Moll, J., Pittalà, V., Roletto, F., Severino, D., Soncini, C., Storici, P., ... Vianello, P. (2005). Potent and selective aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition. Journal of Medicinal Chemistry, 48(8), 3080-3084. https://doi.org/10.1021/jm049076m