Inhibition of eEF2-K by thieno[2,3-b]pyridine analogues.

Basic Information

ID: ALA1156286

Journal: Bioorg Med Chem Lett

Title: Inhibition of eEF2-K by thieno[2,3-b]pyridine analogues.

Authors: Lockman JW, Reeder MD, Suzuki K, Ostanin K, Hoff R, Bhoite L, Austin H, Baichwal V, Adam Willardsen J.

Abstract: Several series of thieno[2-3-b]pyridine analogues were synthesized and screened for inhibitory activity against eukaryotic elongation factor-2 kinase (eEF2-K). Modifications around several regions of the lead molecules were made, with a ring fusion adjacent to the nitrogen on the thienopyridine core being critical for activity. The most active compound 34 shows an IC(50) of 170 nM against eEF2-K in vitro.

CiteXplore: 20189382

DOI: 10.1016/j.bmcl.2010.02.005

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