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ID: ALA1125933

Journal: J Med Chem

Title: Arocalciferols: synthesis and biological evaluation of aromatic side-chain analogues of 1 alpha,25-dihydroxyvitamin D3(1a).

Authors: Figadère B, Norman AW, Henry HL, Koeffler HP, Zhou JY, Okamura WH.

Abstract: Aromatic side-chain analogues (arocalciferols 6-9) of the steroid hormone 1 alpha,25-dihydroxyvitamin D3 (1) were synthesized and biologically evaluated. The analogues were prepared by coupling the vitamin D A-ring enyne 14 with the appropriate enol triflate of a modified CD steroid fragment of the type 22. The resulting dienyne 23 was then transformed in three steps to the vitamin D analogues 6-9. Biological evaluation of these analogues have provided information concerning side-chain topographical effects on in vivo and in vitro activity.

CiteXplore: 1652020

DOI: 10.1021/jm00112a021