Abstract
The syntheses and biological profiles of sulfoximine-based Vioxx analogs 2 are described. Interesting data have been obtained for 2a, which shows a selective COX-2 inhibition (albeit not as strong as Vioxx itself) exhibiting reduced hERG activity compare to the parent sulfone Vioxx (1).
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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Cyclooxygenase 2 / metabolism*
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Cyclooxygenase 2 Inhibitors / chemical synthesis
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Cyclooxygenase 2 Inhibitors / chemistry
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Cyclooxygenase 2 Inhibitors / pharmacology*
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Dose-Response Relationship, Drug
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Ether-A-Go-Go Potassium Channels / antagonists & inhibitors*
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HEK293 Cells
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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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Methionine Sulfoximine / analogs & derivatives
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Methionine Sulfoximine / chemistry
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Methionine Sulfoximine / pharmacology*
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Molecular Structure
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Stereoisomerism
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Structure-Activity Relationship
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Sulfones / chemical synthesis
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Sulfones / chemistry
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Sulfones / pharmacology*
Substances
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Cyclooxygenase 2 Inhibitors
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Ether-A-Go-Go Potassium Channels
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Lactones
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Sulfones
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rofecoxib
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Methionine Sulfoximine
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Cyclooxygenase 2
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PTGS2 protein, human