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

2013; Elsevier BV; Volume: 23; Issue: 11 Linguagem: Inglês

10.1016/j.bmcl.2013.03.109

1464-3405

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

Synthesis of heterocyclic compounds

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.