The guareschi pyridine scaffold as a valuable platform for the identification of selective PI3K inhibitors

Ubaldina Galli, Elisa Ciraolo, Alberto Massarotti, Jean Piero Margaria, Giovanni Sorba, Emilio Hirsch, Gian Cesare Tron

Risultato della ricerca: Contributo su rivistaArticolo in rivistapeer review

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 originaleInglese
pagine (da-a)17275-17287
Numero di pagine13
RivistaMolecules
Volume20
Numero di pubblicazione9
DOI
Stato di pubblicazionePubblicato - 1 set 2015

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