Portal de Periódicos da CAPES

Efficient and Versatile Synthesis of Novel 2α-Substituted 1α,25-Dihydroxyvitamin D 3 Analogues and Their Docking to Vitamin D Receptors

2001; American Chemical Society; Volume: 66; Issue: 26 Linguagem: Inglês

10.1021/jo010375i

1520-6904

Yoshitomo Suhara, Ken‐ichi Nihei, Masaaki Kurihara, Atsushi Kittaka, Kentaro Yamaguchi, Toshie Fujishima, Katsuhiro Konno, Naoki Miyata, Hiroaki Takayama,

Estrogen and related hormone effects

Novel 2alpha-substituted 1alpha,25-dihydroxyvitamin D(3) analogues with 2alpha-alkyl and 2alpha-hydroxyalkyl groups were systematically synthesized from D-xylose. Their conformation on binding to the ligand binding domain (LBD) of the vitamin D receptor was analyzed. It has been found that the 2alpha-hydroxypropyl group best fits the cavity of the LBD, and the binding activity is three times higher than that for the natural hormone.