769126-80-9Relevant academic research and scientific papers
The 2α-(3-hydroxypropyl) group as an active motif in vitamin D3 analogues as agonists of the mutant vitamin D receptor (Arg274Leu)
Honzawa, Shinobu,Yamamoto, Yasuhiro,Yamashita, Atsushi,Sugiura, Takayuki,Kurihara, Masaaki,Arai, Midori A.,Kato, Shigeaki,Kittaka, Atsushi
, p. 3002 - 3024 (2008/09/20)
We designed and synthesized 1α- and 1β-hydroxymethyl-2α-(3-hydroxypropyl)-25-hydroxyvitamin D3 (2a,b) and related analogues 2α-(3-hydroxypropyl)-25-hydroxyvitamin D3 (3), Posner's analogues of 1α- and 1β-hydroxymethyl-25-hydroxyvitamin D3 (4a,b), as well as 2α-(3-hydroxypropyl)-1α,25-dihydroxyvitamin D3 (5), to confirm the effect of the 1α-hydroxy group and/or 2α-(3-hydroxypropyl) group of vitamin D3 analogues with the modified A-ring moiety on the mutant vitamin D receptor, VDR(Arg274Leu). The 2α-(3-hydroxypropyl) group showed better effect on enhancement of the transcriptional activity through the mutant VDR than the 1α- and 1β-hydroxymethyl groups.
24,24-Dimethylvitamin D3-26,23-lactones and their 2α-functionalized analogues as highly potent VDR antagonists
Saito, Nozomi,Masuda, Manami,Matsunaga, Toshihiro,Saito, Hiroshi,Anzai, Miyuki,Takenouchi, Kazuya,Miura, Daishiro,Ishizuka, Seiichi,Takimoto-Kamimura, Midori,Kittaka, Atsushi
, p. 7951 - 7961 (2007/10/03)
Novel vitamin D receptor (VDR) antagonists, 24,24-dimethyl-1α- hydroxyvitamin D3-26,23-lactones (8 and 9) and their C2α functionalized analogues (8a-c and 9a-c) were efficiently synthesized and their biological activities were evaluated. The co
