Discovery of a novel class of pyridine derivatives that selectively inhibits mutant isocitrate dehydrogenase 2.

Abstract excerpt

This paper presents synthesis and structure-activity relationship of pyridine derivatives as inhibitors of mutant isocitrate dehydrogenase 2 (IDH2). A series of 2,4,6-trisubstituted pyridine derivatives have been prepared and evaluated in vitro. Among these compounds, 14n exhibited excellent inhibition activity with the IC50 of 54.6 nm, which is approximately onefold improvement compared to drug candidate AG-221...

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