Pyridone-containing farnesyltransferase inhibitors: Synthesis and biological evaluation

Farnesyltransferase inhibitors (FTIs) have been developed as potential anti-cancer agents due to their efficacy in blocking malignant growth in a variety of murine models of human tumors. To that end, we have developed a series of pyridone farnesyltransferase inhibitors with potent in vitro and cellular activity. The synthesis, SAR and biological properties of these compounds will be discussed. (C) 2003 Elsevier Ltd. All rights reserved.