title: Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors.
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.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. ashwin.rao@merck.com
authors.forename: Ashwin U
authors.initials: AU
authors.lastname: Rao
authors.forename: Dong
authors.initials: D
authors.lastname: Xiao
authors.forename: Xianhai
authors.initials: X
authors.lastname: Huang
authors.forename: Wei
authors.initials: W
authors.lastname: Zhou
authors.forename: James
authors.initials: J
authors.lastname: Fossetta
authors.forename: Dan
authors.initials: D
authors.lastname: Lundell
authors.forename: Fang
authors.initials: F
authors.lastname: Tian
authors.forename: Prashant
authors.initials: P
authors.lastname: Trivedi
authors.forename: Robert
authors.initials: R
authors.lastname: Aslanian
authors.forename: Anandan
authors.initials: A
authors.lastname: Palani
mesh_terms: D001381:Azepines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D047908:Intracellular Signaling Peptides and Proteins / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D010079:Oxazocines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D000099190:MAP-Kinase-Activated Kinase 2
chemical_list: D001381:Azepines; D047908:Intracellular Signaling Peptides and Proteins; D010079:Oxazocines; D047428:Protein Kinase Inhibitors; D017346:Protein Serine-Threonine Kinases; D000099190:MAP-Kinase-Activated Kinase 2