Inhibition of eEF2-K by thieno[2,3-b]pyridine analogues.
| Autor: | Lockman JW; Department of Medicinal Chemistry, Myriad Pharmaceuticals, 305 Chipeta Way, Salt Lake City, UT 84108, United States. jeffrey.lockman@myriadpharma.com, Reeder MD, Suzuki K, Ostanin K, Hoff R, Bhoite L, Austin H, Baichwal V, Adam Willardsen J |
|---|---|
| Jazyk: | angličtina |
| Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Apr 01; Vol. 20 (7), pp. 2283-6. Date of Electronic Publication: 2010 Feb 06. |
| DOI: | 10.1016/j.bmcl.2010.02.005 |
| Abstrakt: | 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. (2010 Elsevier Ltd. All rights reserved.) |
| Databáze: | MEDLINE |
| Externí odkaz: |
|
Full Text from ScienceDirect