2. Academic Validation
  3. Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors

Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors

  • Bioorg Med Chem Lett. 2012 Jan 15;22(2):1068-72. doi: 10.1016/j.bmcl.2011.11.113.
Ashwin U Rao 1,  Dong Xiao,  Xianhai Huang,  Wei Zhou,  James Fossetta,  Dan Lundell,  Fang Tian,  Prashant Trivedi,  Robert Aslanian,  Anandan Palani
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. ashwin.rao@merck.com
PMID: 22182499 DOI: 10.1016/j.bmcl.2011.11.113
Abstract

Facile synthesis of two new series of tetracyclic azepine and oxazocine analogs is described. These analogs were evaluated for their potential as MAPKAP-K2 (MK2) inhibitors and several were found to be potent at inhibiting MK2 with a non-ATP competitive binding mode.

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