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Oxepinamides: Novel Liver X Receptor Agonists from Aspergillus puniceus
Author(s) -
Lu XinHua,
Shi QingWen,
Zheng ZhiHui,
Ke AiBing,
Zhang Hua,
Huo ChangHong,
Ma Ying,
Ren Xiao,
Li YeYing,
Lin Jie,
Jiang Qin,
Gu YuCheng,
Kiyota Hiromasa
Publication year - 2011
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201000812
Subject(s) - chemistry , liver x receptor , stereochemistry , aspergillus , receptor , nuclear receptor , biochemistry , transcription factor , gene , microbiology and biotechnology , biology
Four novel oxepin‐containing pyrimidines, namely oxepinamides D–G ( 1 – 4 ), were isolated from cultures of Aspergillus puniceus F02Z‐1744. The structures of 1 – 4 were elucidated by analyzing their spectroscopic data generated by 1D and 2D NMR and MS methods. The configurations of 1 and 2 were established based on single‐crystal X‐ray crystallographic analysis. All four compounds 1 – 4 showed transcriptional activation on Liver X Receptor α (LXRα) with EC 50 values of 10.6, 12.8, 13.6, and 12.1 μ M , respectively.