Design, Synthesis, and Evaluation of Novel Modular Bisubstrate Analogue Inhibitors of Farnesyltransferase

Promising potential chemotherapeutics for the treatment of cancer can be developed from farnesyltransferase inhibitors. A novel class of modular bisubstrate farnesyltransferase inhibitors is presented that can be synthesized in a straightforward manner. An example of such an inhibitor is compound 1, which has an IC₅₀ value of 3.7 μM.