This technology includes a novel chemotype against mutant (R 132H) isocitrate dehydrogenase 1 (IDH1) enzyme to be utilized as an anticancer therapy. We have progressed the structure activity relationship (SAR) and optimized the compound to be low nanomolar inhibitor of the enzyme with low nanomolar inhibition of the target in cells. These compounds lower 2-hydroxyglutarate, which has been termed an 'oncometabolite' and is common in a subset of cancers including glioma, cholangiocarcinoma, chondrosarcoma and acute myeloid leukemia.