Abstract
Sulfoximine-based acyclic triaryl olefins 8 and 9 have been prepared and initial studies have been performed to determine their biological profiles. In contrast to their sulfonyl-substituted analog 2 sulfoximines 8 and 9 show low COX inhibitory activity. All compounds affect the estrogen receptors. While sulfone 2 interacts exclusively with ER β, sulfoximines 8 and 9 reveal almost equal blocking potencies for both estrogen receptors, ER α and ER β. In the tested series, triaryl olefin 9a shows the highest inhibitory activities with 91% and 80%, respectively (at 10 μM).
Copyright © 2012 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkenes / chemical synthesis
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Alkenes / chemistry*
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Alkenes / pharmacology
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Cyclooxygenase 1 / chemistry
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Cyclooxygenase 1 / metabolism
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Cyclooxygenase 2 / chemistry
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Cyclooxygenase 2 / metabolism
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Cyclooxygenase Inhibitors / chemical synthesis*
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Cyclooxygenase Inhibitors / chemistry
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Cyclooxygenase Inhibitors / pharmacology
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Estrogen Receptor alpha / antagonists & inhibitors
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Estrogen Receptor alpha / metabolism
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Estrogen Receptor beta / antagonists & inhibitors
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Estrogen Receptor beta / metabolism
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Humans
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Imines / chemistry*
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Protein Binding / drug effects
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Sulfones / chemistry
Substances
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Alkenes
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Anti-Inflammatory Agents, Non-Steroidal
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Cyclooxygenase Inhibitors
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Imines
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Sulfones
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Cyclooxygenase 1
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Cyclooxygenase 2