Surfing the piperazine core of tricyclic farnesyltransferase inhibitors

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.

An ECLiPS® library, containing 11,718 compounds, was used to explore the structure–activity relationships surrounding the piperazine core of tricyclic farnesyltransferase inhibitors. Compounds 6 and 9, with IC50s of less than 50 nM, are representative of the most potent structures identified from the screen.Figure optionsDownload as PowerPoint slide