Abstract
Novel vitamin D 3 analogs having a lactam structure in their side chains, 1α,25-dihydroxyvitamin D 3-26,23-lactams (DLAMs), were designed based on the principle of regulation of the folding of helix-12 in the vitamin D nuclear receptor (VDR). The new analogs were synthesized via 1,3-dipolar cycloaddition reaction and subsequent reduction of the isoxazolidine as key steps. Among the analogs, (23 S,25 S)-DLAM-01 ( 4a) and (23 S,25 S)-DLAM-1P ( 5a) bind strongly to VDR. Moreover, these analogs were found to inhibit the differentiation of HL-60 cells induced by 1α,25-dihydroxyvitamin D 3.
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