Towards a RIOK2 chemical probe: cellular potency improvement of a selective 2-(acylamino)pyridine series
Literature Information
Publication Date
2020-11-11
DOI
10.1039/D0MD00292E
Impact Factor
0
Authors
Álvaro Lorente-Macías
View Original
Abstract
RIOK2 is an understudied kinase associated with a variety of human cancers including non-small cell lung cancer and glioblastoma. No potent, selective, and cell-active chemical probe currently exists for RIOK2. Such a reagent would expedite re-search into the biological functions of RIOK2 and validate it as a therapeutic target. Herein, we describe the synthesis of naphthyl–pyridine based compounds that have improved cellular activity while maintaining selectivity for RIOK2. While our compounds do not represent RIOK2 chemical probes, they are the best available tool molecules to begin to characterize RIOK2 function in vitro.
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