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Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase. |
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| Authors: | D C Beshore I M Bell C J Dinsmore C F Homnick J C Culberson R G Robinson C Fernandes E S Walsh M T Abrams H G Bhimnathwala J P Davide M S Ellis-Hutchings H A Huber K S Koblan C A Buser N E Kohl R B Lobell I W Chen D A McLoughlin T V Olah S L Graham G D Hartman T M Williams |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, PA 19486, West Point, USA. douglas_beshore@merck.com |
| 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. |
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