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    Tetrahydrobenzothiophene carboxamides: Beyond the kinase domain and into the fatty acid realm.

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    Date
    2017-Sep
    Author
    Sabin Llona-Minguez
    Shabnam Fayezi
    Alireza Alihemmati
    Jordi Juárez-Jiménez
    F Javier Piedrafita
    Thomas Helleday
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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.
    DOI
    http://dx.doi.org/S0960-894X(17)30795-3
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