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
  • 1. Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. [email protected]
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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