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.
Lingua originale | Inglese |
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pagine (da-a) | 17275-17287 |
Numero di pagine | 13 |
Rivista | Molecules |
Volume | 20 |
Numero di pubblicazione | 9 |
DOI | |
Stato di pubblicazione | Pubblicato - 1 set 2015 |