254445-87-9Relevant academic research and scientific papers
Inhibitors of prenyl-protein transferase
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, (2008/06/13)
The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds
Evaluation of amino acid-based linkers in potent macrocyclic inhibitors of farnesyl-protein transferase
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.
, p. 1817 - 1821 (2007/10/03)
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.
