2. Academic Validation
  3. Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition

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

  • J Med Chem. 2005 Apr 21;48(8):3080-4. doi: 10.1021/jm049076m.
Daniele Fancelli 1,  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 Tonani,  Mario Varasi,  Anna Vulpetti,  Paola Vianello
Affiliations

Affiliation

  • 1 Nerviano Medical Sciences - Oncology, via Pasteur 10, 20014 Nerviano, Milan, Italy. [email protected]
PMID: 15828847 DOI: 10.1021/jm049076m
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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