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

…, SR Cho, M Koh, WK Oh, HS Choi, SB Park

文献索引：Koo, Ja Young; Oh, Sangmi; Cho, Seung-Rye; Koh, Minseob; Oh, Won-Keun; Choi, Hueng-Sik; Park, Seung Bum Organic and Biomolecular Chemistry, 2013 , vol. 11, # 35 p. 5782 - 5786

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被引用次数: 1

摘要

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.