title: Surfing the piperazine core of tricyclic farnesyltransferase inhibitors.
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.
authors.affiliation: Pharmacopeia, PO Box 5350, Princeton, NJ 08543-5350, USA. rock@pcop.com
authors.forename: Laura L
authors.initials: LL
authors.lastname: Rokosz
authors.forename: Chia-Yu
authors.initials: CY
authors.lastname: Huang
authors.forename: John C
authors.initials: JC
authors.lastname: Reader
authors.forename: Tara M
authors.initials: TM
authors.lastname: Stauffer
authors.forename: Daniel
authors.initials: D
authors.lastname: Chelsky
authors.forename: Nolan H
authors.initials: NH
authors.lastname: Sigal
authors.forename: Ashit K
authors.initials: AK
authors.lastname: Ganguly
authors.forename: John J
authors.initials: JJ
authors.lastname: Baldwin
mesh_terms: D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D051231:Farnesyltranstransferase / Q000037:antagonists & inhibitors*; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology; D007700:Kinetics; D010879:Piperazines / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D007093:Imidazoles; D010879:Piperazines; D051231:Farnesyltranstransferase