Synthesis and biological evaluation of 4-substituted vitamin d and 14-epi-previtamin d analogs.
We synthesized the 4-hydroxy and 4-methoxy analogs of active vitamin D(3) (1alpha,25(OH)(2)D(3), 1) and its C14-epimer with the previtamin D(3) form of 14-epi-1alpha,25(OH)(2)preD(3) (14-epi-pre1). Their vitamin D receptor (VDR) binding affinity and osteocalcin promoter transactivation activity in HOS cells were evaluated, and had lower activity than the natural hormone (1) and 14-epi-pre1, respectively.
Sawada
Daisuke
D
Teikyo University, Sagamiko, Kanagawa, Japan.
Tsukuda
Yuya
Y
Saito
Hiroshi
H
Takagi
Ken-ichiro
K
Horie
Kyouhei
K
Ochiai
Eiji
E
Takenouchi
Kazuya
K
Kittaka
Atsushi
A
D001665:Binding Sites; D002762:Cholecalciferol / Q000138:chemical synthesis* / Q000235:genetics / Q000378:metabolism; D006801:Humans; D015394:Molecular Structure; D010006:Osteoblasts / Q000378:metabolism; D018167:Receptors, Calcitriol / Q000737:chemistry / Q000378:metabolism; D014807:Vitamin D / Q000031:analogs & derivatives* / Q000737:chemistry
D018167:Receptors, Calcitriol; D014807:Vitamin D; D002762:Cholecalciferol