Synthetic studies of vitamin D analogues. IX. Synthesis and differentiation-inducing activity of 1 alpha,25-dihydroxy-23-oxa-, thia-, and azavitamin D3. |
| |
| Authors: | N Kubodera K Miyamoto M Akiyama M Matsumoto T Mori |
| |
| Institution: | Exploratory Research Laboratories, Chugai Pharmaceutical Co., Ltd., Shizuoka, Japan. |
| |
| Abstract: | Three vitamin D3 analogues, 1 alpha,25-dihydroxy-23-oxavitamin D3 (3), 1 alpha,25-dihydroxy-23-thiavitamin D3 (4) and 1 alpha,25-dihydroxy-23-azavitamin D3 (5) were synthesized. In the differentiation-inducing activity of human myeloid leukemia cells into macrophages in vitro, the 23-aza analogue (5) showed the least activity, while no remarkable differences were observed between the 23-oxa analogue (3) and the 23-thia analogue (4), which were less active than 1 alpha,25-dihydroxyvitamin D3 (1). |
| |
| Keywords: | |
|
|
