Effect of structural modification on the inhibitory selectivity of rutaecarpine derivatives on human CYP1A1, CYP1A2, and CYP1B1.

Abstract:

:Derivatives of a CYP1A2 inhibitor rutaecarpine were synthesized to have potent and selective inhibition of human CYP1 members. Structural modelling shows a good fitting of rutaecarpine with the putative active site of human CYP1A2. Among the derivatives, 10- and 11-methoxyrutaecarpine are the most selective CYP1B1 inhibitors. 1-Methoxyrutaecarpine and 1,2-dimethoxyrutaecarpine are the most selective CYP1A2 inhibitors.

journal_name

Bioorg Med Chem Lett

authors

Don MJ,Lewis DF,Wang SY,Tsai MW,Ueng YF

doi

10.1016/s0960-894x(03)00469-4

subject

Has Abstract

pub_date

2003-08-04 00:00:00

pages

2535-8

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960894X03004694

journal_volume

13

pub_type

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