Download MendeleyPotent and Selective Aurora Inhibitors Identified by the Expansion of a Novel Scaffold for Protein Kinase Inhibition.
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., Pittala, V., Roletto, F., Severino, D., Soncini, C., Storici, P., Tonani, R., Varasi, M., Vulpetti, A., Vianello, P.(2005) J Med Chem 48: 3080
- PubMed: 15828847
- DOI: https://doi.org/10.1021/jm049076m
- Primary Citation of Related Structures:
2BMC - PubMed 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.
Organizational Affiliation:
Nerviano Medical Sciences - Oncology, via Pasteur 10, 20014 Nerviano, Milan, Italy. [email protected]
