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  • An o-aminoanilide analogue of 1α,25-dihydroxyvitamin D(3) functions as a strong vitamin D receptor antagonist.

An o-aminoanilide analogue of 1α,25-dihydroxyvitamin D(3) functions as a strong vitamin D receptor antagonist.

Journal of medicinal chemistry (2010-10-05)
Marc Lamblin, Russell Spingarn, Tian-Tian Wang, Melanie C Burger, Basel Dabbas, Nicolas Moitessier, John H White, James L Gleason
ABSTRACT

Vitamin D receptor (VDR) antagonists have therapeutic potential in treatment of allergic conditions and hypercalcemia driven by granulomatous diseases. We have identified an o-aminoanilide analogue of the hormonal form of vitamin D with a dienyl side chain that functions as a strong VDR antagonist. Modeling studies indicate that antagonism arises from side chain rigidity, when compared to a more flexible saturated analogue, which interferes with H12 folding/alignment.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
1α,25-Dihydroxyvitamin D3, ≥99% (HPLC)
Sigma-Aldrich
1α,25-Dihydroxyvitamin D3, ≥97.0% (HPLC)
Sigma-Aldrich
1α,25-Dihydroxyvitamin D2 solution, 100 μg/mL in ethanol, 95% (CP)
Sigma-Aldrich
1α,25-Dihydroxyvitamin D2 solution, 50 μg/mL in ethanol, 95% (CP)