Surfing the piperazine core of tricyclic farnesyltransferase inhibitors

Autor:	Nolan H. Sigal, Daniel Chelsky, Chia-Yu Huang, Ashit K. Ganguly, Laura L. Rokosz, Tara M. Stauffer, Baldwin John J, John C. Reader
Rok vydání:	2005
Předmět:	chemistry.chemical_classification Farnesyl-diphosphate farnesyltransferase biology Stereochemistry High-throughput screening Farnesyltransferase Organic Chemistry Clinical Biochemistry Imidazoles Pharmaceutical Science Biochemistry Piperazines Kinetics Structure-Activity Relationship Piperazine chemistry.chemical_compound Scintillation proximity assay chemistry Drug Discovery biology.protein Farnesyltranstransferase Molecular Medicine Enzyme Inhibitors Molecular Biology Tricyclic
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 15:5537-5543
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::098f79bc54654d556ec79f95ae0ec813 https://doi.org/10.1016/j.bmcl.2005.08.074 Zobrazit plný text záznamu Full Text from ScienceDirect