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Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.
Beshore, D C; Bell, I M; Dinsmore, C J; Homnick, C F; Culberson, J C; Robinson, R G; Fernandes, C; Walsh, E S; Abrams, M T; Bhimnathwala, H G; Davide, J P; Ellis-Hutchings, M S; Huber, H A; Koblan, K S; Buser, C A; Kohl, N E; Lobell, R B; Chen, I W; McLoughlin, D A; Olah, T V; Graham, S L; Hartman, G D; Williams, T M.
Bioorg Med Chem Lett ; 11(14): 1817-21, 2001 Jul 23.
Article in English | MEDLINE | ID: mdl-11459639

ABSTRACT

A series of amino acid-based linkers was used to investigate the effects of various substituents upon the potency, pharmacokinetic properties, and conformation of macrocyclic farnesyl-protein transferase inhibitors (FTIs). As a result of the studies described herein, highly potent FTIs with improved pharmacokinetic profiles have been identified.


Subject(s)
Alkyl and Aryl Transferases/antagonists & inhibitors , Alkyl and Aryl Transferases/drug effects , Enzyme Inhibitors/administration & dosage , Enzyme Inhibitors/pharmacokinetics , Amino Acids/chemistry , Animals , Cells, Cultured , Dogs , Enzyme Inhibitors/chemical synthesis , Half-Life , Inhibitory Concentration 50 , Metabolic Clearance Rate/physiology , Molecular Conformation , Protein Binding/drug effects , Rats
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