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Bioorg Med Chem Lett. 2013 Jun 1;23(11):3262-6. doi: 10.1016/j.bmcl.2013.03.109. Epub 2013 Apr 4.

Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.

Author information

1
Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. dong.xiao@merck.com

Abstract

Conformation restriction of linear N-alkylanilide MK2 inhibitors to their E-conformer was developed. This strategy enabled rapid advance in identifying a series of potent non-ATP competitive inhibitors that exhibited cell based activity in anti-TNFα assay.

PMID:
23602398
DOI:
10.1016/j.bmcl.2013.03.109
[Indexed for MEDLINE]

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