Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374574 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
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 IC50 of 170 nM against eEF2-K in vitro.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jeffrey W. Lockman, Matthew D. Reeder, Kazuyuki Suzuki, Kirill Ostanin, Ryan Hoff, Leena Bhoite, Harry Austin, Vijay Baichwal, J. Adam Willardsen,