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ID: ALA2384992

Journal: Bioorg Med Chem Lett

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

Authors: Xiao D, Palani A, Huang X, Sofolarides M, Zhou W, Chen X, Aslanian R, Guo Z, Fossetta J, Tian F, Trivedi P, Spacciapoli P, Whitehurst CE, Lundell D.

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.

CiteXplore: 23602398

DOI: 10.1016/j.bmcl.2013.03.109