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Molecules 2015, 20(9), 17275-17287; doi:10.3390/molecules200917275

The Guareschi Pyridine Scaffold as a Valuable Platform for the Identification of Selective PI3K Inhibitors

1
Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale "A. Avogadro", Largo Donegani 2, Novara 28100, Italy
2
Department of Molecular Biotechnology and Health Sciences, Molecular Biotechnology Center, University of Torino, Via Nizza 52, Torino 10126, Italy
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: James W. Leahy
Received: 13 July 2015 / Revised: 9 September 2015 / Accepted: 14 September 2015 / Published: 18 September 2015
(This article belongs to the Special Issue Kinase Inhibitor Chemistry)
View Full-Text   |   Download PDF [1414 KB, uploaded 18 September 2015]   |  

Abstract

A novel series of 4-aryl-3-cyano-2-(3-hydroxyphenyl)-6-morpholino-pyridines have been designed as potential phosphatidylinositol-3-kinase (PI3K) inhibitors. The compounds have been synthesized using the Guareschi reaction to prepare the key 4-aryl-3-cyano-2,6-dihydroxypyridine intermediate. A different selectivity according to the nature of the aryl group has been observed. Compound 9b is a selective inhibitor against the PI3Kα isoform, maintaining a good inhibitory activity. Docking studies were also performed in order to rationalize its profile of selectivity. View Full-Text
Keywords: PI3 kinase; pyridine; Guareschi reaction; isoforms; selectivity PI3 kinase; pyridine; Guareschi reaction; isoforms; selectivity
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MDPI and ACS Style

Galli, U.; Ciraolo, E.; Massarotti, A.; Margaria, J.P.; Sorba, G.; Hirsch, E.; Tron, G.C. The Guareschi Pyridine Scaffold as a Valuable Platform for the Identification of Selective PI3K Inhibitors. Molecules 2015, 20, 17275-17287.

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