Cancer
Cell culture studies identified a pteridinylbenzamide-based dual PLK1/BRD4 inhibitor that could help treat AML. Chemical synthesis and screening of analogs of a pteridinylbenzamide-based tool compound PLK1 inhibitor in enzyme activity assays yielded a compound that inhibited PLK1 and BRD4 with IC50 values of 28 and 40 nM, respectively. In a human AML cell line, the compound increased the percentage of cells arrested at the G1 and G2 cell cycle stages compared with vehicle. Next steps in collaboration with Novartis AG could include testing the compound in animal models of AML.
Nerviano Medical Sciences s.r.l. and Trovagene Inc. have onvansertib (PMC-075; NMS-1286937; NMS-P937), an oral PLK1 selective inhibitor, in Phase II testing for AML and prostate cancer and Phase I for solid tumors...