367268-96-0Relevant articles and documents
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 (2004)
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.
