Bioorganic and Medicinal Chemistry Letters p. 1817 - 1821 (2001)
Update date:2022-08-02
Topics:
Beshore, Douglas C.
Bell, Ian M.
Dinsmore, Christopher J.
Homnick, Carl F.
Culberson
Robinson, Ronald G.
Fernandes, Christine
Walsh, Eileen S.
Abrams, Marc T.
Bhimnathwala, Hema G.
Davide, Joseph P.
Ellis-Hutchings, Michelle S.
Huber, Hans A.
Koblan, Kenneth S.
Buser, Carolyn A.
Kohl, Nancy E.
Lobell, Robert B.
Chen, I-Wu
McLoughlin, Debra A.
Olah, Timothy V.
Graham, Samuel L.
Hartman, George D.
Williams, Theresa M.
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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