335160-95-7Relevant academic research and scientific papers
Macrocyclic piperazinones as potent dual inhibitors of farnesyltransferase and geranylgeranyltransferase-I
Dinsmore, Christopher J.,Zartman, C. Blair,Bergman, Jeffrey M.,Abrams, Marc T.,Buser, Carolyn A.,Culberson, J. Christopher,Davide, Joseph P.,Ellis-Hutchings, Michelle,Fernandes, Christine,Graham, Samuel L.,Hartman, George D.,Huber, Hans E.,Lobell, Robert B.,Mosser, Scott D.,Robinson, Ronald G.,Williams, Theresa M.
, p. 639 - 643 (2007/10/03)
A series of macrocyclic piperazinone compounds with dual farnesyltransferase/geranylgeranyltransferase-I inhibitory activity was prepared. These compounds were found to be potent inhibitors of protein prenylation in cell culture. A hypothesis for the binding mode of compound 3o in FPTase is proposed.
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 of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
3,8-Diazabicyclo[3.2.1]octan-2-one peptide mimetics: synthesis of a conformationally restricted inhibitor of farnesyltransferase.
Dinsmore,Bergman,Bogusky,Culberson,Hamilton,Graham
, p. 865 - 868 (2007/10/03)
A new synthesis of the 3,8-diazabicyclo[3.2.1]octan-2-one framework is described. Transannular enolate alkylation of piperazinone derivatives provides a flexible route to highly constrained bicyclic peptidomimetic synthons with substitution at the Calpha
