TY - JOUR
T1 - Tetrahydrobenzothiophene carboxamides
T2 - Beyond the kinase domain and into the fatty acid realm
AU - Llona-Minguez, Sabin
AU - Fayezi, Shabnam
AU - Alihemmati, Alireza
AU - Juárez-Jiménez, Jordi
AU - Piedrafita, F. Javier
AU - Helleday, Thomas
N1 - Publisher Copyright:
© 2017 Elsevier Ltd
PY - 2017
Y1 - 2017
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=85028301296&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2017.08.006
DO - 10.1016/j.bmcl.2017.08.006
M3 - Journal articles
C2 - 28807439
AN - SCOPUS:85028301296
SN - 0960-894X
VL - 27
SP - 4462
EP - 4466
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 18
ER -