New low-density lipoprotein receptor upregulators acting via a novel mechanism

MJ Ashton, TJ Brown, G Fenton, F Halley…

文献索引：Ashton, Michael J.; Brown, Thomas J.; Fenton, Garry; Halley, Frank; Harper, Mark F.; Lockey, Peter M.; Porter, Barry; Roach, Alan G.; Stuttle, Keith A. J.; Vicker, Nigel; Walsh, Roger J. A. Journal of Medicinal Chemistry, 1996 , vol. 39, # 17 p. 3343 - 3356

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被引用次数: 16

摘要

The synthesis and biological activity of a new series of benzamides and related compounds that upregulate the expression of the low-density lipoprotein (LDL) receptor in human hepatocytes (HepG2 cells) by a novel mechanism are described. The lead compound, N-[5- [(3-cyclohexylpropionyl) amino]-2-methylphenyl]-4-hydroxybenzamide (1, RPR102359), increased the expression of the LDL receptors in HepG2 cells by 80% when tested at a ...