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Bioorg Med Chem Lett ; 11(10): 1257-60, 2001 May 21.
Article in English | MEDLINE | ID: mdl-11392531

ABSTRACT

Imidazolemethyl diaryl ethers are potent inhibitors of farnesyl-protein transferase. The SNAr displacement reaction used to prepare these diaryl ethers was amenable to rapid parallel synthesis of FPTase inhibitors. The use of a broad range of commercially available phenols quickly identified compounds which proved active in cells.


Subject(s)
Alkyl and Aryl Transferases/antagonists & inhibitors , Phenyl Ethers/pharmacology , Alkyl and Aryl Transferases/metabolism , Animals , Binding, Competitive , Cell Line , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/pharmacology , Imidazoles/chemistry , Inhibitory Concentration 50 , Peptide Library , Phenyl Ethers/chemical synthesis , Rats , Structure-Activity Relationship
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