Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14α-demethylase (CYP51)

…, M Seliškar, D Kocjan, KF Tacer, D Rozman…

Index: Korosec, Tina; Acimovic, Jure; Seliskar, Matej; Kocjan, Darko; Tacer, Klementina Fon; Rozman, Damjana; Urleb, Uros Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 1 p. 209 - 221

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Citation Number: 29

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 14α-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.