Issue 35, 2013
From the journal:

Organic & Biomolecular Chemistry

Total synthesis of eryvarin H and its derivatives and their biological activity as ERRγ inverse agonist†

Ja Young Koo,a   Sangmi Oh,b   Seung-Rye Cho,c   Minseob Koh,a   Won-Keun Oh,d   Hueng-Sik Choi*c  and  Seung Bum Park*ae  

* Corresponding authors

a Department of Chemistry, Seoul National University, Seoul, Korea
E-mail: sbpark@snu.ac.kr

b Medicinal Chemistry Team, Institut Pasteur Korea, Seongnam-si, Gyeonggi-do 463-400, Korea

c National Creative Research Initiatives Center for Nuclear Receptor Signals, Hormone Research Center, School of Biological Sciences and Technology, Chonnam National University, Gwangju 500-757, Korea
E-mail: hsc@chonnam.ac.kr

d College of Pharmacy, Seoul National University, Seoul 151-742, Korea

e Department of Biophysics and Chemical Biology/Bio-MAX Institute, Seoul National University, Seoul 151-747, Korea
E-mail: sbpark@snu.ac.kr

Abstract

Total synthesis of eryvarin H and a biological investigation of its analogues as a potential inverse agonist of ERRγ are described here. Among the 13 analogues prepared by the modular synthetic route, eryvarin H and compound 12 showed meaningful ERRγ inverse agonistic activities along with moderate selectivity over ERα and other nuclear receptors in the cell-based reporter gene assay.

Graphical abstract: Total synthesis of eryvarin H and its derivatives and their biological activity as ERRγ inverse agonist

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Article information

DOI
https://doi.org/10.1039/C3OB41264D
Article type
Communication
Submitted
19 Jun 2013
Accepted
12 Jul 2013
First published
17 Jul 2013

Org. Biomol. Chem., 2013,11, 5782-5786

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Total synthesis of eryvarin H and its derivatives and their biological activity as ERRγ inverse agonist

J. Y. Koo, S. Oh, S. Cho, M. Koh, W. Oh, H. Choi and S. B. Park, Org. Biomol. Chem., 2013, 11, 5782 DOI: 10.1039/C3OB41264D

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