Tetrahydrobenzothiophene carboxamides: Beyond the kinase domain and into the fatty acid realm. Issue 18 (15th September 2017)

• Record Type: Journal Article
• Authors: Llona-Minguez, Sabin; Fayezi, Shabnam; Alihemmati, Alireza; Juárez-Jiménez, Jordi; Piedrafita, F. Javier; Helleday, Thomas
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 18(2017)
• Page Start: 4462
• Page End: 4466
• Publication Date: 2017-09-15
• Subjects: Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.08.006
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A series of tetrahydrobenzothiophene carboxamides, inspired by structural features present in kinase and SCD1 inhibitors, are presented here. Prototype compound8 (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.