Abstract
A series of cyclopentane derivatives was synthesized and evaluated for inhibition of the steroid metabolizing enzymes AKR1C1 and AKR1C3. Selective inhibitors that are active in the low micromolar range were identified. These compounds represent promising starting points in the development of new anticancer agents for the treatment of hormone-dependent forms of cancer and other diseases where AKR1C1 and AKR1C3 are involved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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20-Hydroxysteroid Dehydrogenases / antagonists & inhibitors*
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3-Hydroxysteroid Dehydrogenases / antagonists & inhibitors*
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Aldo-Keto Reductase Family 1 Member C3
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Computer Simulation
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Cyclopentanes / chemical synthesis
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Cyclopentanes / chemistry
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Cyclopentanes / pharmacology*
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Dose-Response Relationship, Drug
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Drug Design
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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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Humans
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Hydroxyprostaglandin Dehydrogenases / antagonists & inhibitors*
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Models, Chemical
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Molecular Conformation
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Cyclopentanes
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Enzyme Inhibitors
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3-Hydroxysteroid Dehydrogenases
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20-Hydroxysteroid Dehydrogenases
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3 alpha-beta, 20 beta-hydroxysteroid dehydrogenase
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Hydroxyprostaglandin Dehydrogenases
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AKR1C3 protein, human
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Aldo-Keto Reductase Family 1 Member C3