Citation:
Hu Daihua, Chen Wang. Advances in Syntheses and Biological Activities of Vitamin D2 Analogues[J]. Chemistry,
;2017, 80(8): 715-724.
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1α, 25-Dihydroxyvitamin D2(1α, 25-(OH)2-D2; 125D2) is the active metabolite form of vitamin D2, and 1α, 25-dihydroxyvitamin D3(1α, 25-(OH)2-D3; 125D) is the most active metabolite of vitamin D3. The biological activity of 125D2 and 125D is similar, but the therapeutic application of 125D is limited by induction of hypercalcemia. Vitamin D2 and analogues are thought to be generally less toxic than the respective vitamin D3 compounds. This article reviews the recent development of two 125D2 analogues (doxercalciferol and paricalcitol) showed good clinical effect in organic syntheses, and new research in the design and syntheses of the structural modifications in the side chain, 19-nor, C3-substituted in A ring, and nonadeuterated isotope labeling 125D2 analogues, and the relation between the structure and the biological activities, aimed at guiding significance to the syntheses and clinical development of new selective biological vitamin D2 analogues.
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