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

Llona-Minguez S, Fayezi S, Alihemmati A, Juárez-Jiménez J, Piedrafita FJ, Helleday T

Bioorg. Med. Chem. Lett. 27 (18) 4462-4466 [2017-09-15; online 2017-08-05]

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.

Affiliated researcher

PubMed 28807439

DOI 10.1016/j.bmcl.2017.08.006

Crossref 10.1016/j.bmcl.2017.08.006

pii: S0960-894X(17)30795-3

Publications 9.5.0