Surfing the piperazine core of tricyclic farnesyltransferase inhibitors.
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.
Rokosz
Laura L
LL
Pharmacopeia, PO Box 5350, Princeton, NJ 08543-5350, USA. rock@pcop.com
Huang
Chia-Yu
CY
Reader
John C
JC
Stauffer
Tara M
TM
Chelsky
Daniel
D
Sigal
Nolan H
NH
Ganguly
Ashit K
AK
Baldwin
John J
JJ
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
D004791:Enzyme Inhibitors; D007093:Imidazoles; D010879:Piperazines; D051231:Farnesyltranstransferase