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Molecules 2015, 20(9), 17275-17287;

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

Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale "A. Avogadro", Largo Donegani 2, Novara 28100, Italy
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)
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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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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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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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