The discovery of C-linked imidazole azaheptapyridine bridgehead FPT inhibitors is described. This novel class of compounds are sub nM FPT enzyme inhibitors with potent cellular inhibitory activities. This series also has reduced hERG activity versus previous N-linked imidazole series. X-ray of compound 10a bound to FTase revealed strong interaction between bridgehead imidazole 3N with catalytic zinc atom.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2009.12.013 | DOI Listing |
Publication Analysis
Top Keywords
fpt inhibitors
8
discovery c-imidazole
4
c-imidazole azaheptapyridine
4
azaheptapyridine fpt
4
inhibitors discovery
4
discovery c-linked
4
c-linked imidazole
4
imidazole azaheptapyridine
4
azaheptapyridine bridgehead
4
bridgehead fpt
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!