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Volume 10
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10.3390/biom10081131
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Article

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

by
Toan Dao-Huy
1,2,
Simone Latkolik
3,
Julia Bräuer
3,
Andreas Pfeil
3,
Hermann Stuppner
4,
Michael Schnürch
1,*,
Verena M. Dirsch
3,* and
Marko D. Mihovilovic
1
1
Institute of Applied Synthetic Chemistry, TU Wien, Getreidemarkt 9/163, 1060 Vienna, Austria
2
Department of Pharmaceutical and Pesticide Technology, School of Chemical Engineering, Hanoi University of Science and Technology, Dai Co Viet 1, Hai Ba Trung dist., Hanoi 10000, Vietnam
3
Department of Pharmacognosy, University of Vienna, Althanstraße 14, 1090 Vienna, Austria
4
Institute of Pharmacy/Pharmacognosy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria
*
Authors to whom correspondence should be addressed.
Biomolecules 2020, 10(8), 1131; https://doi.org/10.3390/biom10081131
Submission received: 7 July 2020 / Revised: 24 July 2020 / Accepted: 27 July 2020 / Published: 31 July 2020
(This article belongs to the Section Natural and Bio-derived Molecules)
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Abstract

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.
Keywords: NF-κB inhibition; natural product; lignans; cross-coupling; C-H activation; direct arylation NF-κB inhibition; natural product; lignans; cross-coupling; C-H activation; direct arylation
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MDPI and ACS Style

Dao-Huy, T.; Latkolik, S.; Bräuer, J.; Pfeil, A.; Stuppner, H.; Schnürch, M.; Dirsch, V.M.; Mihovilovic, M.D. Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes. Biomolecules 2020, 10, 1131. https://doi.org/10.3390/biom10081131

AMA Style

Dao-Huy T, Latkolik S, Bräuer J, Pfeil A, Stuppner H, Schnürch M, Dirsch VM, Mihovilovic MD. Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes. Biomolecules. 2020; 10(8):1131. https://doi.org/10.3390/biom10081131

Chicago/Turabian Style

Dao-Huy, Toan, Simone Latkolik, Julia Bräuer, Andreas Pfeil, Hermann Stuppner, Michael Schnürch, Verena M. Dirsch, and Marko D. Mihovilovic. 2020. "Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes" Biomolecules 10, no. 8: 1131. https://doi.org/10.3390/biom10081131

APA Style

Dao-Huy, T., Latkolik, S., Bräuer, J., Pfeil, A., Stuppner, H., Schnürch, M., Dirsch, V. M., & Mihovilovic, M. D. (2020). Structural Features Defining NF-κB Inhibition by Lignan-Inspired Benzofurans and Benzothiophenes. Biomolecules, 10(8), 1131. https://doi.org/10.3390/biom10081131

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