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    Bioorg Med Chem Lett. 2008 Aug 1;18(15):4287-90. Epub 2008 Jul 3.

    Structure-activity relationship studies on vitamin D lactam derivatives as vitamin D receptor antagonist.

    Cho K, Uneuchi F, Kato-Nakamura Y, Namekawa J, Ishizuka S, Takenouchi K, Nagasawa K.

    Department of Biotechnology and Life Science, Faculty of Technology, Tokyo University of Agriculture and Technology, 2-24-16, Naka-cho, Koganei, Tokyo 184-8588, Japan.

    Structure-activity relationship studies on 1alpha,25-dihydroxyvitamin D(3)-26,23-lactams (DLAMs), antagonists of vitamin D, were conducted, focusing on the substituents of the phenyl group. One of the derivatives (23S,25S)-DLAM-1P-3,5(OEt)(2), showed potent antagonistic activity with an IC(50) of 90nM.

    PMID: 18635349 [PubMed - indexed for MEDLINE]

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