1350561-75-9Relevant academic research and scientific papers
S-farnesyl-thiopropionic acid triazoles as potent inhibitors of isoprenylcysteine carboxyl methyltransferase
Bergman, Joel A.,Hahne, Kalub,Song, Jiao,Hrycyna, Christine A.,Gibbs, Richard A.
supporting information; experimental part, p. 15 - 19 (2012/03/27)
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 analogue is a potent inhibitor of Icmt (IC50 = 0.8 ± 0.1 μM; calculated Ki = 0.4 μM).
