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Discovery of bicyclic pyrazoles as class III histone deacetylase SIRT1 and SIRT2 inhibitors.
Therrien, Eric; Larouche, Guillaume; Nguyen, Natalie; Rahil, Jubrail; Lemieux, Anne-Marie; Li, Zuomei; Fournel, Marielle; Yan, Theresa P; Landry, Anne-Julie; Lefebvre, Sylvain; Wang, James J; MacBeth, Kyle; Heise, Carla; Nguyen, Aaron; Besterman, Jeffrey M; Déziel, Robert; Wahhab, Amal.
Afiliação
  • Therrien E; Department of Medicinal Chemistry, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada. Electronic address: eric@molecularforecaster.com.
  • Larouche G; Department of Medicinal Chemistry, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • Nguyen N; Department of Medicinal Chemistry, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • Rahil J; Department of Lead Discovery, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • Lemieux AM; Department of Lead Discovery, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • Li Z; Department of Molecular Biology, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • Fournel M; Department of Molecular Biology, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • Yan TP; Department of Molecular Biology, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • Landry AJ; Department of Molecular Biology, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • Lefebvre S; Department of Molecular Biology, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • Wang JJ; Department of Molecular Biology, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • MacBeth K; Celgene Inc., 4550 Towne Centre Court, San Diego, CA 92121, United States.
  • Heise C; Celgene Inc., 4550 Towne Centre Court, San Diego, CA 92121, United States.
  • Nguyen A; Celgene Inc., 4550 Towne Centre Court, San Diego, CA 92121, United States.
  • Besterman JM; Department of Molecular Biology, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • Déziel R; Department of Medicinal Chemistry, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
  • Wahhab A; Department of Medicinal Chemistry, MethylGene Inc., 7150 rue Frederick-Banting, Montreal, QC H4S 2A1, Canada.
Bioorg Med Chem Lett ; 25(12): 2514-8, 2015 Jun 15.
Article em En | MEDLINE | ID: mdl-25971769
ABSTRACT
A series of bicyclic pyrazole carboxamides was synthesized and tested for inhibitory activity against the class III deacetylase sirtuin enzymes. Moderate to low micromolar inhibitory activities were obtained against SIRT1 and SIRT2. These bicyclic pyrazole compounds represent a new class of sirtuin inhibitors with a preference for SIRT1 over SIRT2.
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Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Pirazóis / Compostos Bicíclicos com Pontes / Sirtuína 1 / Sirtuína 2 Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article
Texto completo
Adicionar na Minha BVS
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Bases de dados: MEDLINE Assunto principal: Pirazóis / Compostos Bicíclicos com Pontes / Sirtuína 1 / Sirtuína 2 Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article