An asymmetric synthesis of two analogues of SL0101 () has been achieved. The effort is aimed at the discovery of inhibitors of the p90 ribosomal S6 kinase (RSK) with improved bioavailability. The route relies upon the use of the Taylor catalyst to regioselectively install -3″ acetyl or carbamate functionality. This study led to the identification of a third-generation analogue of SL0101 with a -4″ -Pr-carbamate and a -3″ acetate with improved RSK inhibitory activity.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7292201 | PMC |
| http://dx.doi.org/10.1021/acs.orglett.0c00042 | DOI Listing |
Publication Analysis
Top Keywords
analogue sl0101
8
regioselective synthesis
4
synthesis -4''
4
-4'' carbamate-6''
4
carbamate-6'' -pr
4
-pr substituted
4
substituted cyclitol
4
cyclitol analogue
4
sl0101 asymmetric
4
asymmetric synthesis
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!