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

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 farnesyltra...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-12, Vol.13 (24), p.4361-4364
Main Authors: ANGIBAUD, Patrick, SAHA, Ashis K, PONCELET, Virginie, ROUX, Bruno, SMETS, Gerda, VAN DUN, Jacky, VENET, Marc, WOUTERS, Walter, BOURDREZ, Xavier, END, David W, FREYNE, Eddy, LEZOURET, Patricia, MANNENS, Geert, MEVELLEC, Laurence, MEYER, Christophe, PILATTE, Isabelle
Format: Article
Language:English
Subjects:
Administration, Oral
Alkyl and Aryl Transferases - antagonists & inhibitors
Animals
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Division - drug effects
Enzyme Inhibitors - administration & dosage
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Farnesyltranstransferase
General aspects
Heterocyclic Compounds - administration & dosage
Heterocyclic Compounds - chemical synthesis
Heterocyclic Compounds - chemistry
Heterocyclic Compounds - pharmacology
Humans
Kinetics
Medical sciences
Mice
Microsomes, Liver - drug effects
Microsomes, Liver - metabolism
Models, Molecular
Molecular Conformation
Pharmacology. Drug treatments
Quinolones - administration & dosage
Quinolones - chemical synthesis
Quinolones - pharmacology
Structure-Activity Relationship
Triazoles - chemical synthesis
Triazoles - chemistry
Triazoles - pharmacology
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.09.043