Synthetic Strategy and Biological Activity of A-ring Stereoisomers of 1,25- Dihydroxyvitamin D 3 and C2-Modified Analogues
2014
The hormonally active form of vitamin D 3 , 1α,25-dihydroxyvitamin D 3 (1a), has a wide variety of biological
activities and its major molecular target is considered to be the vitamin D receptor (VDR). The A-ring stereoisomers of 1a
as well as its C2-modified analogues, which have different stereochemistry at the C1 and/or C3 hydroxy groups, are of interest
since recent metabolic studies have shown that catabolism could occur through A-ring modification. In this review,
a practical and versatile synthesis of the A-ring enyne precursors by the convergent method of Trost and coworkers, which
is needed to construct all possible A-ring stereoisomers of 1,25-dihydroxyvitamin D 3 (1a-d), and the C2-modified analogues
(4a-d, 5a-d, 6a-d and 7a-d) is described. A strategy for the synthesis and evaluation of all possible A-ring stereoisomers
of 1a and their A-ring modified analogues is important, and this will stimulate synthesis and biological studies into
vitamin D.
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