6 alpha,7 alpha-cyclopropane derivatives of androst-4-ene: a novel class of competitive aromatase inhibitors

6 alpha,7 alpha-Cyclopropane steroids were found to be potent competitive inhibitors of human placental aromatase. 6 beta,7 beta-Dihydro-3'H-cyclopropa [6,7]-androst-4-en-17-one (4) has extremely high affinity for aromatase (Ki = 5 nM) but does not cause a time-dependent inactivation of the enz...

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Bibliographic Details
Published inBiochemical and biophysical research communications Vol. 177; no. 1; pp. 401 - 406
Main Authors Numazawa, M, Mutsumi, A
Format Journal Article
LanguageEnglish
Published United States 31.05.1991
Subjects
Androstenedione
Androstenes - chemical synthesis
Androstenes - pharmacology
Aromatase Inhibitors
Binding, Competitive
Cyclopropanes - chemical synthesis
Cyclopropanes - pharmacology
Female
Humans
Indicators and Reagents
Kinetics
Microsomes - enzymology
Placenta - enzymology
Pregnancy
Structure-Activity Relationship
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Summary:6 alpha,7 alpha-Cyclopropane steroids were found to be potent competitive inhibitors of human placental aromatase. 6 beta,7 beta-Dihydro-3'H-cyclopropa [6,7]-androst-4-en-17-one (4) has extremely high affinity for aromatase (Ki = 5 nM) but does not cause a time-dependent inactivation of the enzyme.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
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ISSN:0006-291X
DOI:10.1016/0006-291X(91)91997-Q