Synthesis of novel C-2 substituted vitamin D derivatives having ringed side chains and their biological evaluation on bone

• Published in: The Journal of steroid biochemistry and molecular biology Vol. 136; pp. 3 - 8
• Main Authors: Saito, Hiroshi, Takagi, Kenichiro, Horie, Kyohei, Kakuda, Shinji, Takimoto-Kamimura, Midori, Ochiai, Eiji, Chida, Takayuki, Harada, Yoshifumi, Takenouchi, Kazuya, Kittaka, Atsushi
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.07.2013
• Subjects: Animals; Bone Density - drug effects; Chemistry Techniques, Synthetic; Crystallography, X-Ray; Female; Human osteosarcoma cell; Humans; Models, Molecular; Molecular Structure; Osteoporosis - drug therapy; Osteoporosis - metabolism; Ovariectomized (OVX) rat model; Rats; Receptors, Calcitriol - chemistry; Receptors, Calcitriol - metabolism; Structure-Activity Relationship; Transactivation; Vitamin D - analogs & derivatives; Vitamin D - chemical synthesis; Vitamin D - pharmacology; Vitamin D analogs; Vitamin D receptor; Vitamin D3; Vitamin D analogs; Vitamin D3; Transactivation; Vitamin D receptor; Human osteosarcoma cell; Ovariectomized (OVX) rat model

▸ We synthesized novel vitamin D3 derivatives with chiral cyclopentanone in the side chain. ▸ Novel derivatives showed strong transactivation activities in spite of weak affinity to VDR. ▸ Some derivatives showed strong activities for enhancing bone growth using OVX therapeutic rats. Up to the prese...