Abstract
The synthesis and structure-activity relationships (SAR) of salubrinal, a small molecule that protects cells from apoptosis induced by endoplasmic reticulum (ER) stress, are described. It is revealed that the trichloromethyl group greatly contributes to the activity. Based on the SAR results, salubrinal was converted into a biotinylated derivative which retains activity and can be used as a biological tool for target identification.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Apoptosis / drug effects
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Biotinylation
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Cell Survival / drug effects
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Cinnamates / chemical synthesis*
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Cinnamates / pharmacology
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Dose-Response Relationship, Drug
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PC12 Cells
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Protective Agents / chemical synthesis*
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Protective Agents / pharmacology
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Rats
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Structure-Activity Relationship
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Thiourea / analogs & derivatives*
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Thiourea / chemical synthesis
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Thiourea / pharmacology
Substances
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Cinnamates
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Protective Agents
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salubrinal
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Thiourea