1439381-79-9Relevant academic research and scientific papers
Synthesis of 2α-heteroarylalkyl active vitamin D3 with therapeutic effect on enhancing bone mineral density in vivo
Matsuo, Miki,Hasegawa, Asami,Takano, Masashi,Saito, Hiroshi,Kakuda, Shinji,Chida, Takayuki,Takagi, Ken-Ichiro,Ochiai, Eiji,Horie, Kyohei,Harada, Yoshifumi,Takimoto-Kamimura, Midori,Takenouchi, Kazuya,Sawada, Daisuke,Kittaka, Atsushi
, p. 671 - 674 (2013/07/26)
2α-Heteroarylethyl-1α,25-dihydroxyvitamin D3 analogues, which were designed to form a hydrogen bond between Arg274 of human vitamin D receptor (hVDR) and a nitrogen atom of the heteroaromatic ring at the 2α-position, were synthesized. Among them, 2α-[2-(tetrazol-2-yl) ethyl]-1α,25-dihydroxyvitamin D3 showed higher osteocalcin promoter transactivation activity in human osteosarcoma (HOS) cells and a greater therapeutic effect in ovariectomized (OVX) rats, osteoporosis model animals, on enhancing bone mineral density than those of active vitamin D 3. X-ray cocrystallographic analysis of the hVDR-ligand complex confirms that the new hydrogen bond formation stabilized the complex.
