Relationship of 25-hydroxyvitamin D3 side chain structure to biological activity.
作者： M F Holick , M Garabedian , H K Schnoes , H F DeLuca
DOI: 10.1016/S0021-9258(19)42004-8
关键词: Renal physiology 、 Side chain 、 Hydroxylation 、 Calcium 、 Endocrinology 、 Internal medicine 、 Biological activity 、 Kidney 、 Calcium metabolism 、 Structure–activity relationship 、 Chemistry
摘要: 27-nor-25-Hydroxyvitamin D3, 26,27-bisnor-25-hydroxyvitamin and 22-27-hexanor-20-hydroxyvitamin D3 the corresponding 5,6-trans isomers have been synthesized. All compounds were tested for their ability to induce intestinal calcium transport bone mobilization in normal anephric rats. The 27-nor- analog are capable of stimulating rats but 10 100 times less active than 25-hydroxyvitamin D3. Although these analogs inactive rats, isomer both intestine activity animals. its incapable either or mobilization. These results suggest that minor alterations side chain significantly decrease biopotency Since biologically not animals, it appears kidney 1alpha-hydroxylation is necessary activity. 22-27-hexanor=20-hydroxyvitamin inactive, likely at least part stimulate
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