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 Tonani; Mario Varasi; Anna Vulpetti; Paola Vianello

doi:10.1021/jm049076m

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

Istituto Europeo di Oncologia

Research output: Contribution to journal › Article › peer-review

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 language	English
Pages (from-to)	3080-3084
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	48
Issue number	8
DOIs	https://doi.org/10.1021/jm049076m
Publication status	Published - Apr 21 2005

ASJC Scopus subject areas

Organic Chemistry

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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

Fancelli, D, Berta, D, Bindi, S, Cameron, A, Cappella, P, Carpinelli, P, Catana, C, Forte, B, Giordano, P, Giorgini, ML, Mantegani, S, Marsiglio, A, Meroni, M, Moll, J, Pittalà, V, Roletto, F, Severino, D, Soncini, C, Storici, P, Tonani, R, Varasi, M, Vulpetti, A & Vianello, P 2005, 'Potent and selective aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition', Journal of Medicinal Chemistry, vol. 48, no. 8, pp. 3080-3084. https://doi.org/10.1021/jm049076m

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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.",

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AU - Fancelli, Daniele

AU - Berta, Daniela

AU - Bindi, Simona

AU - Cameron, Alexander

AU - Cappella, Paolo

AU - Carpinelli, Patrizia

AU - Catana, Cornel

AU - Forte, Barbara

AU - Giordano, Patrizia

AU - Giorgini, Maria Laura

AU - Mantegani, Sergio

AU - Marsiglio, Aurelio

AU - Meroni, Maurizio

AU - Moll, Juergen

AU - Pittalà, Valeria

AU - Roletto, Fulvia

AU - Severino, Dino

AU - Soncini, Chiara

AU - Storici, Paola

AU - Tonani, Roberto

AU - Varasi, Mario

AU - Vulpetti, Anna

AU - Vianello, Paola

PY - 2005/4/21

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

Abstract

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