title: Solid-phase synthesis of novel inhibitors of farnesyl transferase.
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.
authors: Cancer Research Campaign Laboratory, CRC Centre for Cancer Therapeutics at the Institute of Cancer Research, Sutton, Surrey, UK.
authors: A M
authors: AM
authors: Barber
authors: I R
authors: IR
authors: Hardcastle
authors: M G
authors: MG
authors: Rowlands
authors: B P
authors: BP
authors: Nutley
authors: J H
authors: JH
authors: Marriott
authors: M
authors: M
authors: Jarman
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051231:Farnesyltranstransferase
chemical_list: D004791:Enzyme Inhibitors; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase