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

Sabin Llona-Minguez; Shabnam Fayezi; Alireza Alihemmati; Jordi Juárez-Jiménez; F. Javier Piedrafita; Thomas Helleday

doi:10.1016/j.bmcl.2017.08.006

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

Sabin Llona-Minguez^*, Shabnam Fayezi, Alireza Alihemmati, Jordi Juárez-Jiménez, F. Javier Piedrafita, Thomas Helleday

^*Korrespondierende/r Autor/-in für diese Arbeit

Klinik für Frauenheilkunde und Geburtshilfe

1 Zitat (Scopus)

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.

Originalsprache	Englisch
Zeitschrift	Bioorganic and Medicinal Chemistry Letters
Jahrgang	27
Ausgabenummer	18
Seiten (von - bis)	4462-4466
Seitenumfang	5
ISSN	0960-894X
DOIs	https://doi.org/10.1016/j.bmcl.2017.08.006
Publikationsstatus	Veröffentlicht - 2017

Fördermittel

We acknowledge Dr. Gaelle Cane for insightful manuscript discussions. This work was supported by the Swedish Research Council, the Knut and Alice Wallenberg Foundation, the G?ran Gustafsson Foundation, the Swedish Pain Relief Foundation, the Torsten S?derbergs Stiftelse, the Swedish Children's Cancer Foundation, and the Swedish Cancer Society. We would also like to acknowledge the Faculty of Medicine at Tabriz University of Medical Sciences for providing research facilities and ChemAxon (http://www.chemaxon.com) for technical support. We acknowledge Dr. Gaelle Cane for insightful manuscript discussions. This work was supported by the Swedish Research Council , the Knut and Alice Wallenberg Foundation , the Göran Gustafsson Foundation , the Swedish Pain Relief Foundation , the Torsten Söderbergs Stiftelse , the Swedish Children’s Cancer Foundation , and the Swedish Cancer Society . We would also like to acknowledge the Faculty of Medicine at Tabriz University of Medical Sciences for providing research facilities and ChemAxon ( http://www.chemaxon.com ) for technical support.

Träger	Trägernummer
G?ran Gustafsson Foundation
Swedish Children's Cancer Foundation
Swedish Children's Cancer Foundation
Swedish Pain Relief Foundation
Torsten Söderbergs Stiftelse
Pain Relief Foundation
Cancerfonden
Göran Gustafssons Stiftelse för Naturvetenskaplig och Medicinsk Forskning
Knut och Alice Wallenbergs Stiftelse
Vetenskapsrådet
Tabriz University of Medical Sciences

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10.1016/j.bmcl.2017.08.006

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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.",

author = "Sabin Llona-Minguez and Shabnam Fayezi and Alireza Alihemmati and Jordi Ju{\'a}rez-Jim{\'e}nez and Piedrafita, \{F. Javier\} and Thomas Helleday",

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AU - Llona-Minguez, Sabin

AU - Fayezi, Shabnam

AU - Alihemmati, Alireza

AU - Juárez-Jiménez, Jordi

AU - Piedrafita, F. Javier

AU - Helleday, Thomas

PY - 2017

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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.

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U2 - 10.1016/j.bmcl.2017.08.006

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M3 - Journal articles

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AN - SCOPUS:85028301296

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EP - 4466

JO - Bioorganic and Medicinal Chemistry Letters

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ER -

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

Abstract

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