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ID: ALA1131955
Journal: Bioorg Med Chem Lett
Title: Solid-phase synthesis of novel inhibitors of farnesyl transferase.
Authors: Barber AM, Hardcastle IR, Rowlands MG, Nutley BP, Marriott JH, Jarman M.
Abstract: A novel diphosphate mimic, the 2,3,6-trifluoro-5-hydroxy-4-nitrophenoxy group (1), has been employed as the template in the solid-phase synthesis of novel farnesyl transferase inhibitors using the Mitsunobu reaction. The most potent inhibitor (farnesyloxy-5-hydroxy-2,3,6-trifluoro-4-nitrobenzene) displayed an IC50 of 6.3 microM versus farnesyl transferase.
CiteXplore: 10098677