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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 |
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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 |
format | article |
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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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