New C15-Substituted Active Vitamin D3

详细信息    查看全文

• 作者：Kanako Shindo ; Go Kumagai ; Masashi Takano ; Daisuke Sawada ; Nozomi Saito ; Hiroshi Saito ; Shinji Kakuda ; Ken-ichiro Takagi ; Eiji Ochiai ; Kyohei Horie ; Midori Takimoto-Kamimura ; Seiichi Ishizuka ; Kazuya Takenouchi ; Atsushi Kittaka
• 刊名：Organic Letters
• 出版年：2011
• 出版时间：June 3, 2011
• 年：2011
• 卷：13
• 期：11
• 页码：2852-2855
• 全文大小：816K
• 年卷期：v.13,no.11(June 3, 2011)
• ISSN：1523-7052

文摘

C15-Substituted 1伪,25-dihydroxyvitamin D₃ analogs were synthesized for the first time to investigate the effects of the modified CD-ring on biological activity concerning the agonistic positioning of helix-3 and helix-12 of the vitamin D receptor (VDR). X-ray cocrystallographic analysis proved that 0.6 脜 shifts of the CD-ring and shrinking of the side chain were necessary to maintain the position of the 25-hydroxy group for proper interaction with helix-12. The 15-hydroxy-16-ene derivative showed higher binding affinity for hVDR than the natural hormone.