Surfing the piperazine core of tricyclic farnesyltransferase inhibitors

Abstract In order to fully explore structure–activity relationships at the 1- and 2-positions of the piperazine core of tricyclic farnesyltransferase inhibitors, an 11,718-member ECLiPS ® library was synthesized and screened in a farnesyltransferase scintillation proximity assay. A detailed description of the library and analyses of the screening data will be provided.