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.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2010.02.005 | DOI Listing |
Publication Analysis
Top Keywords
inhibition eef2-k
4
eef2-k thieno[23-b]pyridine
4
thieno[23-b]pyridine analogues
4
analogues series
4
series thieno[2-3-b]pyridine
4
thieno[2-3-b]pyridine analogues
4
analogues synthesized
4
synthesized screened
4
screened inhibitory
4
inhibitory activity
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!