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Bioorg Med Chem Lett ; 15(24): 5537-43, 2005 Dec 15.
Article in English | MEDLINE | ID: mdl-16202593

ABSTRACT

In order to fully explore structure-activity relationships at the 1- and 2-positions of the piperazine core of tricyclic farnesyltransferase inhibitors, an 11,718-member ECLiPS library was synthesized and screened in a farnesyltransferase scintillation proximity assay. A detailed description of the library and analyses of the screening data will be provided.


Subject(s)
Enzyme Inhibitors/chemistry , Farnesyltranstransferase/antagonists & inhibitors , Piperazines/chemistry , Piperazines/pharmacology , Enzyme Inhibitors/pharmacology , Imidazoles/chemistry , Imidazoles/pharmacology , Kinetics , Structure-Activity Relationship
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