Selective cytochrome P450 3A4 inhibitory activity of Amaryllidaceae alkaloids.

Abstract:

:A library of natural and semi-synthetic Amaryllidaceae alkaloids was screened for cytochrome P450 3A4 (CYP3A4) inhibitory activity. Of the crinane, lycorane and galanthamine representatives examined two semi-synthetic silylated lycorane analogues, accessed via a chemoselective silylation strategy from lycorine, and the natural compound narciclasine exhibited low micromolar activities. Important pharmacological features uncovered include the lack of CYP3A4 inhibitory activity seen for galanthamine and the selective activity that is seen with narciclasine over pancratistatin.

journal_name

Bioorg Med Chem Lett

authors

McNulty J,Nair JJ,Singh M,Crankshaw DJ,Holloway AC,Bastida J

doi

10.1016/j.bmcl.2009.04.086

subject

Has Abstract

pub_date

2009-06-15 00:00:00

pages

3233-7

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00600-3

journal_volume

19

pub_type

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