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  • Title: Dramatic enhancement of antagonistic activity on vitamin D receptor: a double functionalization of 1alpha-hydroxyvitamin D3 26,23-lactones.
    Author: Saito N, Saito H, Anzai M, Yoshida A, Fujishima T, Takenouchi K, Miura D, Ishizuka S, Takayama H, Kittaka A.
    Journal: Org Lett; 2003 Dec 11; 5(25):4859-62. PubMed ID: 14653692.
    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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