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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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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
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cited_by cdi_FETCH-LOGICAL-c329t-6cb7640e6699c6fa3851105ae6d0f651c8bd0d3bda1c443669f909d5551c8e693
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container_end_page 4364
container_issue 24
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container_title Bioorganic & medicinal chemistry letters
container_volume 13
creator 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
description 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.
doi_str_mv 10.1016/j.bmcl.2003.09.043
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identifier ISSN: 0960-894X
ispartof Bioorganic & medicinal chemistry letters, 2003-12, Vol.13 (24), p.4361-4364
issn 0960-894X
1464-3405
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source ScienceDirect Freedom Collection 2022-2024
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
title 4-Methyl-1,2,4-triazol-3-yl heterocycle as an alternative to the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA
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