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

Xiao, Dong; Palani, Anandan; Huang, Xianhai; Sofolarides, Michael; Zhou, Wei; Chen, Xiao; Aslanian, Robert; Guo, Zhuyan; Fossetta, James; Tian, Fang; Trivedi, Prashant; Spacciapoli, Peter; Whitehurst, Charles E; Lundell, Daniel

Xiao, Dong; Palani, Anandan; Huang, Xianhai; Sofolarides, Michael; Zhou, Wei; Chen, Xiao; Aslanian, Robert; Guo, Zhuyan; Fossetta, James; Tian, Fang; Trivedi, Prashant; Spacciapoli, Peter; Whitehurst, Charles E; Lundell, Daniel.

Affiliation

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

Bioorg Med Chem Lett ; 23(11): 3262-6, 2013 Jun 01.

Article in En | MEDLINE | ID: mdl-23602398

Subject(s)

Anilides/chemistry; Intracellular Signaling Peptides and Proteins/antagonists & inhibitors; Lactams/chemistry; Protein Kinase Inhibitors/chemistry; Protein Serine-Threonine Kinases/antagonists & inhibitors; Adenosine Triphosphate/chemistry; Adenosine Triphosphate/metabolism; Anilides/chemical synthesis; Anilides/metabolism; Binding, Competitive; Drug Evaluation, Preclinical; Humans; Intracellular Signaling Peptides and Proteins/metabolism; Lactams/chemical synthesis; Lactams/metabolism; Protein Binding; Protein Kinase Inhibitors/chemical synthesis; Protein Kinase Inhibitors/metabolism; Protein Serine-Threonine Kinases/metabolism; Stereoisomerism; Structure-Activity Relationship

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Full text: 1 Database: MEDLINE Main subject: Protein Serine-Threonine Kinases / Intracellular Signaling Peptides and Proteins / Protein Kinase Inhibitors / Lactams / Anilides Language: En Journal: Bioorg Med Chem Lett Year: 2013 Type: Article Affiliation country: United States

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