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Article

Synthesis and Evaluation of (1,4-Disubstituted)-1,2,3-triazoles as Estrogen Receptor Beta Agonists

1
Department of Chemistry, Marquette University, P.O. Box 1881, Milwaukee, WI 53201-1881, USA
2
School of Pharmacy, Center for Structure-Based Drug Design and Development, Concordia University Wisconsin, Mequon, WI 53097, USA
*
Author to whom correspondence should be addressed.
Academic Editor: Roman B. Lesyk
Sci. Pharm. 2022, 90(3), 46; https://doi.org/10.3390/scipharm90030046
Received: 11 July 2022 / Revised: 24 July 2022 / Accepted: 27 July 2022 / Published: 1 August 2022
(This article belongs to the Special Issue Feature Papers in Scientia Pharmaceutica)
Estrogen receptors (ER) are nuclear hormone receptors which are responsible for sex hormone signaling in women. A series of (1,4-disubstituted)-1,2,3-triazoles 521 were prepared by reaction of azidophenols with terminal alkynes under Fokin reaction conditions. The products were purified by column chromatography or recrystallization and characterized by NMR and HRMS. The compounds were tested for binding to ERβ via a ligand displacement assay, and 1-(4-hydroxyphenyl)-α-phenyl-1,2,3-triazole-4-ethanol (21) was found to be the most potent analog (EC50 = 1.59 μM). Molecular docking of 521 within the ligand binding pocket of ERβ (pdb 2jj3) was performed and the docking scores exhibited a general qualitative trend consistent with the measured EC50 values. View Full-Text
Keywords: estrogen receptor ligand; alkyne–azide cycloaddition; molecular docking estrogen receptor ligand; alkyne–azide cycloaddition; molecular docking
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MDPI and ACS Style

Wetzel, E.A.; Corriero, G.C.; Brown-Ford, S.; Sem, D.S.; Donaldson, W.A. Synthesis and Evaluation of (1,4-Disubstituted)-1,2,3-triazoles as Estrogen Receptor Beta Agonists. Sci. Pharm. 2022, 90, 46. https://doi.org/10.3390/scipharm90030046

AMA Style

Wetzel EA, Corriero GC, Brown-Ford S, Sem DS, Donaldson WA. Synthesis and Evaluation of (1,4-Disubstituted)-1,2,3-triazoles as Estrogen Receptor Beta Agonists. Scientia Pharmaceutica. 2022; 90(3):46. https://doi.org/10.3390/scipharm90030046

Chicago/Turabian Style

Wetzel, Edward A., Grace C. Corriero, Sandra Brown-Ford, Daniel S. Sem, and William A. Donaldson. 2022. "Synthesis and Evaluation of (1,4-Disubstituted)-1,2,3-triazoles as Estrogen Receptor Beta Agonists" Scientia Pharmaceutica 90, no. 3: 46. https://doi.org/10.3390/scipharm90030046

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