Abstract
Structure-activity relationship studies on 1alpha,25-dihydroxyvitamin D(3)-26,23-lactams (DLAMs), antagonists of vitamin D, were conducted, focusing on the substituents of the phenyl group. One of the derivatives (23S,25S)-DLAM-1P-3,5(OEt)(2), showed potent antagonistic activity with an IC(50) of 90nM.
MeSH terms
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Calcitriol / analogs & derivatives*
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Calcitriol / chemical synthesis
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Calcitriol / pharmacokinetics
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Calcitriol / pharmacology
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Combinatorial Chemistry Techniques
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Drug Design
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Humans
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Inhibitory Concentration 50
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Lactams / chemical synthesis
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Lactams / pharmacokinetics
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Lactams / pharmacology*
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Molecular Structure
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Receptors, Calcitriol / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
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Vitamin D / analogs & derivatives*
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Vitamin D / chemical synthesis
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Vitamin D / pharmacokinetics
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Vitamin D / pharmacology
Substances
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DLAM-1P compound
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Lactams
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Receptors, Calcitriol
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Vitamin D
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Calcitriol