An o-Aminoanilide Analogue of 1 alpha,25-Dihydroxyvitamin D-3 Functions as a Strong Vitamin D Receptor Antagonist

作者：Lamblin Marc; Spingarn Russell; Wang Tian Tian; Burger Melanie C; Dabbas Basel; Moitessier Nicolas; White John H^*; Gleason James L

来源：Journal of Medicinal Chemistry, 2010, 53(20): 7461-7465.

DOI：10.1021/jm1007159

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.

• 出版日期2010-10-28