Design and synthesis of seco-oxysterol analogs as potential inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase gene transcription

SD Larsen, CH Spilman, Y Yagi, DM Dinh…

文献索引：Larsen; Spilman; Yagi; Dinh; Hart; Hess Journal of Medicinal Chemistry, 1994 , vol. 37, # 15 p. 2343 - 2351

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被引用次数: 19

摘要

The synthesis and biological activity of a series of seco-oxysterol analogs designed to be inhibitors of transcription of the gene for 3-hydroxy-3-methylglutaryl-Coenzyme A reductase (HMGR) are described. The compound possessing the most significant activity,[la (E), 4/3]-3- [2-(4-hydroxy-l-methylcyclohexyl) etenyll-a, a-dimethylbe~ enepen~ ol (4, U-88156), inhibited (IC50= 10 pM) the expression of/3-galactosidase (/3-gal) in a transfected human ...