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

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

Bioorganic & Medicinal Chemistry Letters（2013）

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摘要

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.

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关键词

Conformation constraint,Alkyl anilide conformation,Non-ATP competitive MK2 inhibitors

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