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

dc.contributor.authorLlona-Minguez, S
dc.contributor.authorFayezi, S
dc.contributor.authorAlihemmati, A
dc.contributor.authorJu?rez-Jimé nez, J
dc.contributor.authorPiedrafita, FJ
dc.contributor.authorHelleday, T
dc.date.accessioned2018-08-26T04:57:21Z
dc.date.available2018-08-26T04:57:21Z
dc.date.issued2017
dc.identifier.urihttp://dspace.tbzmed.ac.ir:8080/xmlui/handle/123456789/38621
dc.description.abstractA 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.
dc.language.isoEnglish
dc.relation.ispartofBioorganic & medicinal chemistry letters
dc.subjectAcetyltransferases
dc.subjectDose-Response Relationship, Drug
dc.subjectEnzyme Inhibitors
dc.subjectFatty Acid Desaturases
dc.subjectFatty Acids
dc.subjectHumans
dc.subjectMolecular Structure
dc.subjectProtein Kinases
dc.subjectStearoyl-CoA Desaturase
dc.subjectStructure-Activity Relationship
dc.subjectThiophenes
dc.titleTetrahydrobenzothiophene carboxamides: Beyond the kinase domain and into the fatty acid realm.
dc.typearticle
dc.citation.volume27
dc.citation.issue18
dc.citation.spage4462
dc.citation.epage4466
dc.citation.indexPubmed
dc.identifier.DOIhttps://doi.org/10.1016/j.bmcl.2017.08.006


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