Tetrahydrobenzothiophene carboxamides: Beyond the kinase domain and into the fatty acid realm |
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| Authors: | Sabin Llona-Minguez Shabnam Fayezi Alireza Alihemmati Jordi Juárez-Jiménez F Javier Piedrafita Thomas Helleday |
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| Institution: | 1. Division of Translational Medicine and Chemical Biology, Science for Life Laboratory, Department of Medical Biochemistry and Biophysics, Karolinska Institutet, Stockholm 171 65, Sweden;2. Department of Biology and Anatomical Sciences, Faculty of Medicine, Shahid Beheshti University of Medical Sciences, Tehran 1983969411, Iran;3. Department of Anatomical Sciences, Faculty of Medicine, Tabriz University of Medical Sciences, Tabriz 5165665931, Iran;4. EaStCHEM School of Chemistry, Joseph Black Building, The King’s Buildings, Edinburgh EH9 3JJ, United Kingdom;5. Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, CA 92121, USA |
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| 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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| Keywords: | Corresponding author |
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