Figure 1.

Structure of tipifarnib: R115777(R)-6-amino[(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolone. Tipifarnib is a farnesyltransferase inhibitor developed by Johnson & Johnson Pharmaceutical Research and Development LLC. It is a nonpeptidomimetic oral quinolone analog of imidazole-containing heterocyclic compounds. It competitively inhibits the CAAX binding site of farnesyl transferase. The imidazole group is the central pharmacophore and the imidazole may interact with the coordination structure of the zinc catalytic site.