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Bioorg Med Chem Lett. 2008 Feb 1;18(3):938-41. doi: 10.1016/j.bmcl.2007.12.037. Epub 2007 Dec 23.

Pyrazinoindolone inhibitors of MAPKAP-K2.

Author information

1
Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc., Research and Development Center, 900 Ridgebury Road, Ridgefield, CT 06877, USA. dgoldber@rdg.boehringer-ingelheim.com

Abstract

Optimization of pyrazinoindolone inhibitors of MAPKAP-K2 (MK2) provides a reasonable balance of cellular potency and physicochemical properties. Mechanistic studies support the inhibition of MK2 which is responsible for the sub-micromolar cellular efficacy.

PMID:
18221871
DOI:
10.1016/j.bmcl.2007.12.037
[Indexed for MEDLINE]

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