Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes

A series of 2-arylbenzofurans and 2-arylbenzothiophenes was synthesized carrying three different side chains in position five. The synthesized compounds were tested for NF-κB inhibition to establish a structure activity relationship. It was found that both, the side chain in position five and the su...

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Autores principales: Dao-Huy, Toan, Latkolik, Simone, Bräuer, Julia, Pfeil, Andreas, Stuppner, Hermann, Schnürch, Michael, Dirsch, Verena M., Mihovilovic, Marko D.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7463992/
https://www.ncbi.nlm.nih.gov/pubmed/32751917
http://dx.doi.org/10.3390/biom10081131
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author Dao-Huy, Toan
Latkolik, Simone
Bräuer, Julia
Pfeil, Andreas
Stuppner, Hermann
Schnürch, Michael
Dirsch, Verena M.
Mihovilovic, Marko D.
author_facet Dao-Huy, Toan
Latkolik, Simone
Bräuer, Julia
Pfeil, Andreas
Stuppner, Hermann
Schnürch, Michael
Dirsch, Verena M.
Mihovilovic, Marko D.
author_sort Dao-Huy, Toan
collection PubMed
description A series of 2-arylbenzofurans and 2-arylbenzothiophenes was synthesized carrying three different side chains in position five. The synthesized compounds were tested for NF-κB inhibition to establish a structure activity relationship. It was found that both, the side chain in position five and the substitution pattern of the aryl moiety in position two have a significant influence on the inhibitory activity.
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spelling pubmed-74639922020-09-04 Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes Dao-Huy, Toan Latkolik, Simone Bräuer, Julia Pfeil, Andreas Stuppner, Hermann Schnürch, Michael Dirsch, Verena M. Mihovilovic, Marko D. Biomolecules Article A series of 2-arylbenzofurans and 2-arylbenzothiophenes was synthesized carrying three different side chains in position five. The synthesized compounds were tested for NF-κB inhibition to establish a structure activity relationship. It was found that both, the side chain in position five and the substitution pattern of the aryl moiety in position two have a significant influence on the inhibitory activity. MDPI 2020-07-31 /pmc/articles/PMC7463992/ /pubmed/32751917 http://dx.doi.org/10.3390/biom10081131 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Dao-Huy, Toan
Latkolik, Simone
Bräuer, Julia
Pfeil, Andreas
Stuppner, Hermann
Schnürch, Michael
Dirsch, Verena M.
Mihovilovic, Marko D.
Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes
title Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes
title_full Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes
title_fullStr Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes
title_full_unstemmed Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes
title_short Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes
title_sort structural features defining nf-κb inhibition by lignan-inspired benzofurans and benzothiophenes
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7463992/
https://www.ncbi.nlm.nih.gov/pubmed/32751917
http://dx.doi.org/10.3390/biom10081131
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