Discovery of a new series of Aurora inhibitors through truncation of GSK1070916

Novel Aurora inhibitors were identified truncating clinical candidate GSK1070916. Many of these truncated compounds retained potent activity against Aurora B with good antiproliferative activity. Mechanistic studies suggested that these compounds, depending on the substitution pattern, may or may not exert their antiproliferative effects via inhibition of Aurora B. The SAR results from this investigation will be presented with an emphasis on the impact structural changes have on the cellular phenotype.

The SAR results from this investigation will be presented with an emphasis on the impact structural changes have on the cellular phenotype.Figure optionsDownload as PowerPoint slide