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Bioorg Med Chem Lett. 2001 Jul 23;11(14):1817-21.

Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase.

Author information

1
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.

PMID:
11459639
DOI:
10.1016/s0960-894x(01)00340-7
[Indexed for MEDLINE]

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