Novel 2α-substituted 1α,25-dihydroxyvitamin D3 analogues were efficiently synthesized and their biological activities were evaluated. 2α-Methyl-1α25-dihydroxyvitamin D3 (2), whose unique biological activities were previously reported, was modified to 2α-alkyl (ethyl and propyl) and 2α-hydroxyalkyl (hydroxymethyl, hydroxyethyl, and hydroxypropyl) analogues 3-7 by elongation of the alkyl chain and/or introduction of a terminal hydroxyl group. 2α-Hydroxypropyl-1α,25-dihydroxyvitamin D3 (7) exhibited an exceptionally potent calcium-regulating effect and a unique activity profile. (C) 2000 Elsevier Science Ltd. All rights reserved.
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