Novel and selective spiroindoline-based inhibitors of Sky kinase.

Bioorg. Med. Chem. Lett.2012 Jan 1;22(1):190-3. Epub 2011 Nov 16

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We report the discovery of a novel series of spiroindoline-based inhibitors of Sky kinase that bind in the ATP-binding site and exhibit high levels of kinome selectivity through filling the Ala571-subpocket. These inhibitors exhibit moderate oral bioavailability in the rat due to low absorption across the gut wall.

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Novel and selective spiroindoline-based inhibitors of Sky kinase.

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