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Bioorg Med Chem Lett. 2003 Aug 4;13(15):2535-8.

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

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1
National Research Institute of Chinese Medicine, 155-1 Li-Nong Street, Sec. 2, Taipei 112, Taiwan, ROC.

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.

PMID:
12852960
DOI:
10.1016/s0960-894x(03)00469-4
[Indexed for MEDLINE]

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