Abstract
A non-estrogenic inhibitor of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) was designed based on a modified 3-hydroxy-estra-1,3,5(10)-triene core having an additional five-member lactone ring and a benzamide group. The inhibitor was synthesized, fully characterized and tested for its ability to inhibit the enzyme activity. Estrogenicity was also investigated and tested on estrogen-dependent T-47D cell line. Interestingly, this steroid derivative showed inhibitory potency towards 17β-HSD1 and did not present residual unwanted estrogenic activity.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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17-Hydroxysteroid Dehydrogenases / antagonists & inhibitors*
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17-Hydroxysteroid Dehydrogenases / metabolism
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Cell Line, Tumor
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Chemistry Techniques, Synthetic
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Dose-Response Relationship, Drug
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Drug Design
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Enzyme Activation / drug effects
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Estradiol / chemistry*
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Humans
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Lactones / chemical synthesis
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Lactones / chemistry
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Lactones / pharmacology*
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Molecular Structure
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Lactones
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Estradiol
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17-Hydroxysteroid Dehydrogenases
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3 (or 17)-beta-hydroxysteroid dehydrogenase