Dramatic enhancement of antagonistic activity on vitamin D receptor: a double functionalization of 1alpha-hydroxyvitamin D3 26,23-lactones |
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Authors: | Saito Nozomi Saito Hiroshi Anzai Miyuki Yoshida Akihiro Fujishima Toshie Takenouchi Kazuya Miura Daishiro Ishizuka Seiichi Takayama Hiroaki Kittaka Atsushi |
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Institution: | Faculty of Pharmaceutical Sciences, Teikyo University, Kanagawa 199-0195, Japan. |
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Abstract: | The synthesis of novel vitamin D receptor antagonists, 24-methyl-1alpha-hydroxyvitamin D(3) 26,23-lactones, is reported. We found that the biological activities of the vitamin D(3) lactones were affected by the structure of the lactone part. Furthermore, introduction of a 2alpha-methyl group into the 24-methylvitamin D(3) lactones dramatically enhanced their anti-vitamin D activity. reaction: see text] |
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