The discovery and optimization of a series of imidazo[1,5-a]pyrazine inhibitors of mTOR is described. HTS hits were optimized for potency, selectivity and metabolic stability to provide the orally bioavailable proof of concept compound 4c that demonstrated target inhibition in vivo and concomitant inhibition of tumor growth in an MDA-MB-231 xenograft model.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2011.01.139 | DOI Listing |
Publication Analysis
Top Keywords
imidazo[15-a]pyrazines orally
4
orally efficacious
4
efficacious inhibitors
4
inhibitors mtorc1
4
mtorc1 mtorc2
4
mtorc2 discovery
4
discovery optimization
4
optimization series
4
series imidazo[15-a]pyrazine
4
imidazo[15-a]pyrazine inhibitors
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!