4-Methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the Farnesyltransferase inhibitor ZARNESTRA ™

Autor:	Patrick Rene Angibaud, Eddy Jean Edgard Freyne, Christophe Meyer, Jacky Van Dun, Gerda Smets, Marc Venet, Isabelle Noëlle Constance Pilatte, Laurence Mevellec, Virginie Sophie Poncelet, Bruno Roux, Geert Mannens, Ashis K. Saha, David William End, Wouters Walter Boudewijn Leopo, Xavier Bourdrez, Patricia Lezouret
Rok vydání:	2003
Předmět:	Models Molecular Stereochemistry Farnesyltransferase Clinical Biochemistry Molecular Conformation Triazole Administration Oral Pharmaceutical Science Antineoplastic Agents Quinolones Biochemistry Mice Structure-Activity Relationship chemistry.chemical_compound Heterocyclic Compounds Drug Discovery Animals Farnesyltranstransferase Humans Imidazole Moiety Enzyme Inhibitors Molecular Biology Alkyl and Aryl Transferases biology Organic Chemistry Farnesyltransferase inhibitor Triazoles Kinetics chemistry Microsomes Liver biology.protein Molecular Medicine Cell Division
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 13:4361-4364
ISSN:	0960-894X
Popis:	Replacement of the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA series by a 4-methyl-1,2,4-triazol-3-yl group gave us compounds with similar structure-activity relationship profiles showing that this triazole is potentially a good surrogate to imidazole for farnesyltransferase inhibition.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::73c04ec35bf3fe1b70503850f6984927 https://doi.org/10.1016/j.bmcl.2003.09.043 Zobrazit plný text záznamu Full Text from ScienceDirect