Abstract
A convergent synthesis to access hydrophobic tail analogs and head group modifications of AAL(S) is described. The analogs synthesised were evaluated for their ability to inhibit ceramide synthase 1 and for their cytotoxicity in K562 cells. Our results have identified inhibitors which are non-cytotoxic yet maintain CerS1 inhibition.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Amino Alcohols / chemical synthesis*
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Amino Alcohols / chemistry
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Amino Alcohols / pharmacology
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Cell Survival / drug effects
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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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Fingolimod Hydrochloride / chemical synthesis*
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Fingolimod Hydrochloride / chemistry
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Fingolimod Hydrochloride / pharmacology
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Humans
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Hydrophobic and Hydrophilic Interactions
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K562 Cells
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Models, Biological
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Molecular Structure
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Oxidoreductases / antagonists & inhibitors*
Substances
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AAL(S) compound
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Amino Alcohols
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Enzyme Inhibitors
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Oxidoreductases
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dihydroceramide desaturase
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Fingolimod Hydrochloride