Structure-activity relationship of 2,4,5-trioxoimidazolidines as inhibitors of thymidine phosphorylase

► Angiogenic thymidine phosphorylase (TP) is a target for cancer chemotherapy. ► Virtual screening of NCI/ACD databases with TP identified imidazolidine inhibitors. ► A series of imidazolidines were prepared and their TP activity evaluated. ► The lead compound was 3-(2,4,5-trioxo-3-phenylethyl-imidazolidin-1-yl)propionamide.