Novel triazole based inhibitors of Ras farnesyl transferase

A novel series of potent inhibitors of Ras farnesyl transferase possessing a 1,2,4-triazole pharmacophore is described. These inhibitors were discovered from a parallel synthesis effort and were subsequently optimized to in vitro IC50 value of less than 1 nM.

A novel series of potent inhibitors of Ras farnesyl transferase possessing a 1,2,4-triazole pharmacophore (5) is described. These inhibitors were discovered from a parallel synthesis effort and were subsequently optimized to in vitro IC50 value of less than 1 nM (19).Figure optionsDownload as PowerPoint slide