SYNTHESIS AND BIOLOGICAL EVALUATION OF 6',7'-DIHYDROXYBERGAMOTTIN (6,7-DHB), A NATURALLY-OCCURRING INHIBITOR OF CYTOCHROME-P450 3A4

Authors
BELLEVUE FH WOSTER PM EDWARDS DJ HE K HOLLENBERG PF
Citation
Fh. Bellevue et al., SYNTHESIS AND BIOLOGICAL EVALUATION OF 6',7'-DIHYDROXYBERGAMOTTIN (6,7-DHB), A NATURALLY-OCCURRING INHIBITOR OF CYTOCHROME-P450 3A4, Bioorganic & medicinal chemistry letters, 7(20), 1997, pp. 2593-2598
Citations number
23
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
20
Year of publication
1997
Pages
2593 - 2598
Database
ISI
SICI code
0960-894X(1997)7:20<2593:SABEO6>2.0.ZU;2-L
Abstract
The recently isolated inhibitor of cytochrome P450 CYP3A4, 6',7'-dihyd roxybergamottin (6,7-DHB), was synthesized by an efficient route that is readily adaptable to the production of analogues. The compound was evaluated as an inhibitor of 3A4 in a purified enzyme preparation, as well as against human liver microsomes and human 3A4 expressed in Esch erichia coil membrane. In each case, 6,7-DHB proved to be a potent NAD PH-and time dependent inactivator of 3A4. (C) 1997 Elsevier Science Lt d.