Oxo-piperazine Derivatives of N-Arylpiperazinones as Inhibitors of Farnesyltransferase

Autor:	I.-W. Chen, Kenneth S. Koblan, George D. Hartman, Robert B. Lobell, Theresa M. Williams, Samuel L. Graham, Jackson B. Gibbs, Ian B Greenberg, Debra A. McLoughlin, Dongming Liu, Jeffrey M. Bergman, Timothy V. Olah, C. Blair Zartman, Donna Wei, Timothy J. O'Neill, Joseph P. Davide, Nancy E. Kohl, Christopher J. Dinsmore
Rok vydání:	2001
Předmět:	Stereochemistry Farnesyltransferase Clinical Biochemistry Pharmaceutical Science Biochemistry Chemical synthesis Piperazines Structure-Activity Relationship chemistry.chemical_compound Dogs Drug Discovery Animals Farnesyltranstransferase Structure–activity relationship Potency Enzyme Inhibitors Molecular Biology Farnesyl-diphosphate farnesyltransferase Alkyl and Aryl Transferases biology Organic Chemistry Piperazine chemistry Enzyme inhibitor biology.protein Lactam Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 11:537-540
ISSN:	0960-894X
DOI:	10.1016/s0960-894x(00)00710-1
Popis:	The evaluation of SAR associated with the insertion of carbonyl groups at various positions of N-arylpiperazinone farnesyltransferase inhibitors is described herein. 1-Aryl-2,3-diketopiperazine derivatives exhibited the best balance of potency and pharmacokinetic profile relative to the parent 1-aryl-2-piperazinones.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d81443e20c905a2a51041cf95b6156e5 https://doi.org/10.1016/s0960-894x(00)00710-1 Zobrazit plný text záznamu Full Text from ScienceDirect