Abstract
A series of novel cyclopropanyl methyl hexadienoic acid retinoids was designed and prepared. These compounds exhibited either selective activity as RXR agonists or pan-agonists on one or more of each of the RAR and RXR isoforms. The most potent pan-agonist 5a (RAR's EC(50)=17-59 nM; RXR's EC(50)=6-14 nM) showed good antiproliferative properties in the in vitro cancer cell lines, ME 180 and RPMI 8226.
MeSH terms
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Binding, Competitive / drug effects
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Cell Differentiation / drug effects
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Cell Division / drug effects
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Cyclopropanes / chemical synthesis*
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Cyclopropanes / pharmacology*
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Humans
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Indicators and Reagents
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Ligands
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Receptors, Retinoic Acid / agonists
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Receptors, Retinoic Acid / drug effects*
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Receptors, Retinoic Acid / genetics
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Sorbic Acid / analogs & derivatives*
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Sorbic Acid / chemical synthesis
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Sorbic Acid / pharmacology
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Transfection
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Tumor Cells, Cultured
Substances
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Cyclopropanes
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Indicators and Reagents
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Ligands
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Receptors, Retinoic Acid
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Sorbic Acid