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.

Download full-text PDF

Source
http://dx.doi.org/10.1016/s0960-894x(01)00340-7DOI Listing

Publication Analysis

Top Keywords

amino acid-based
8
acid-based linkers
8
farnesyl-protein transferase
8
evaluation amino
4
linkers potent
4
potent macrocyclic
4
macrocyclic inhibitors
4
inhibitors farnesyl-protein
4
transferase series
4
series amino
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!