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Tetrahydrobenzothiophene carboxamides: Beyond the kinase domain and into the fatty acid realm.
Llona-Minguez, Sabin; Fayezi, Shabnam; Alihemmati, Alireza; Juárez-Jiménez, Jordi; Piedrafita, F Javier; Helleday, Thomas.
Afiliación
  • Llona-Minguez S; Division of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm 171 65, Sweden. Electronic address: sabin.llona.minguez@scilifelab.se.
  • Fayezi S; Department of Biology and Anatomical Sciences, Faculty of Medicine, Shahid Beheshti University of Medical Sciences, Tehran 1983969411, Iran.
  • Alihemmati A; Department of Anatomical Sciences, Faculty of Medicine, Tabriz University of Medical Sciences, Tabriz 5165665931, Iran.
  • Juárez-Jiménez J; EaStCHEM School of Chemistry, Joseph Black Building, The King's Buildings, Edinburgh EH9 3JJ, United Kingdom.
  • Piedrafita FJ; Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, CA 92121, USA.
  • Helleday T; Division of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm 171 65, Sweden.
Bioorg Med Chem Lett ; 27(18): 4462-4466, 2017 09 15.
Article en En | MEDLINE | ID: mdl-28807439
ABSTRACT
A series of tetrahydrobenzothiophene carboxamides, inspired by structural features present in kinase and SCD1 inhibitors, are presented here. Prototype compound 8 (MMDD13) modulates fatty acid elongase and desaturase indexes, lipid accumulation, while preserving kinase inhibitory activity. This chemotype represents a stepping stone towards chemical probes to study the consequences of lipid metabolism modulation through non-redundant pathways.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proteínas Quinasas / Estearoil-CoA Desaturasa / Tiofenos / Inhibidores Enzimáticos / Ácidos Grasos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Proteínas Quinasas / Estearoil-CoA Desaturasa / Tiofenos / Inhibidores Enzimáticos / Ácidos Grasos Límite: Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article