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Farnesyltransferase (FTase) is a key enzyme that catalyzes the farnesylation of Ras protein. It is used to bind RAS protein to plasma membrane to complete signal transduction. Ras has been shown to be closely related to the development of many cancers. In recent years, FTase has been studied more deeply as an anticancer target. And more and more novel FTase inhibitors have been reported for the treatment of pancreatic cancer, lung cancer, colon cancer, HGPS, PL and so on. This review summarizes the structural features and biological activities of various novel FTase inhibitors reported since 2013. The reported novel FTase inhibitors were reclassified from the perspective of structure, their current tumor antagonism potential was summarized, and their current challenges and future development trends were further analyzed. [ABSTRACT FROM AUTHOR]