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ID: ALA1143909

Journal: Bioorg Med Chem

Title: Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14alpha-demethylase (CYP51).

Authors: Korosec T, Acimovic J, Seliskar M, Kocjan D, Tacer KF, Rozman D, Urleb U.

Abstract: Novel cholesterol biosynthesis inhibitors, a group of pyridylethanol(phenylethyl)amine derivatives, were synthesized. Sterol profiling assay in the human hepatoma HepG2 cells revealed that compounds target human lanosterol 14alpha-demethylase (CYP51). Structure-activity relationship study of the binding with the overexpressed human CYP51 indicates that the pyridine binds within the heme binding pocket in an analogy with the azoles.

CiteXplore: 17964172

DOI: 10.1016/j.bmc.2007.10.001