title: S-Farnesyl-Thiopropionic Acid (FTPA) Triazoles as Potent Inhibitors of Isoprenylcysteine Carboxyl Methyltransferase.
abstract: We report the design and synthesis of novel FTPA-triazole compounds as potent inhibitors of isoprenylcysteine carboxyl methyltransferase (Icmt), through a focus on thioether and isoprenoid mimetics. These mimetics were coupled utilizing a copper-assisted cycloaddition to assemble the potential inhibitors. Using the resulting triazole from the coupling as an isoprenyl mimetic resulted in the biphenyl substituted FTPA triazole 10n. This lipid-modified analog is a potent inhibitor of Icmt (IC(50) = 0.8 ± 0.1 μM; calculated K(i) = 0.4 μM).
authors: Department of Medicinal Chemistry and Molecular Pharmacology and the Center for Cancer Research, Purdue University, West Lafayette, IN 47907, USA.
authors: Joel A
authors: JA
authors: Bergman
authors: Kalub
authors: K
authors: Hahne
authors: Jiao
authors: J
authors: Song
authors: Christine A
authors: CA
authors: Hrycyna
authors: Richard A
authors: RA
authors: Gibbs