Record Display for the EPA National Library Catalog

RECORD NUMBER: 593 OF 1241

OLS Field Name OLS Field Data
Main Title Inhibition of Aromatase Cytochrome P-450 (Estrogen Synthetase) by Derivatives of alpha-Naphthoflavone.
Author Kellis, J. T. ; Nesnow, S. ; Vickery, L. E. ;
CORP Author Health Effects Research Lab., Research Triangle Park, NC. ;California Univ., Irvine. Dept. of Physiology and Biophysics.
Year Published 1986
Report Number EPA/600/J-86/376;
Stock Number PB87-203154
Additional Subjects Enzymes ; Edocrinology ; Cytochromes ; Inhibitors ; Biochemistry ; Naphthols ; Carcinogens ; Steroids ; Reprints ;
Holdings
Library Call Number Additional Info Location Last
Modified
Checkout
Status
NTIS  PB87-203154 Most EPA libraries have a fiche copy filed under the call number shown. Check with individual libraries about paper copy. NTIS 06/21/1988
Collation 7p
Abstract
alpha-Naphthoflavone (ANF; 7,8-benzoflavone) is a potent competitive inhibitor of human aromatase cytochrome P-450 (J.T. Kellis, Jr. and L.E. Vickery, Science 225, 1032 (1984)). The authors have further investigated inhibition of aromatase by several derivatives of ANF. Using human placental microsomes and 40nM and androstenedione as substrate, the compounds tested and their I sub 50 values were: ANF, 0.07 microM; 2-(2-naphthyl)-4H-naphtho 1,2b pyran-4-one, 1.0 microM; 7,8-benzoisoflavone,identical with 100 microM; and 2-phenyl-4Hnaphtho 1,2b furan, > 100 microM. These findings show the necessity of the keto group of ANF in its binding to the enzyme and the importance of size and position of substitution of the exocyclic phenyl ring. (Copyright (C) Pergamon Journals, Ltd.)