Bioorganic and Medicinal Chemistry Letters p. 2593 - 2598 (1997)
Update date:2022-08-11
Topics:
Bellevue III, Frank H.
Woster, Patrick M.
Edwards, David J.
He, Kan
Hollenberg, Paul F.
The recently isolated inhibitor of cytochrome P450 CYP3A4, 6',7'-dihydroxybergamottin (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 Escherichia coil membrane. In each case, 6,7-DHB proved to be a potent NADPH- and time dependent inactivator of 3A4.
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