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Bioorg Med Chem Lett. 2012 Jan 1;22(1):190-3. doi: 10.1016/j.bmcl.2011.11.036. Epub 2011 Nov 16.

Novel and selective spiroindoline-based inhibitors of Sky kinase.

Author information

1
Pfizer Global Research & Development, Michigan Laboratories, Ann Arbor, MI 48105, USA. napowell@comcast.net

Abstract

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.

PMID:
22119469
DOI:
10.1016/j.bmcl.2011.11.036
[Indexed for MEDLINE]

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