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ID: ALA1155889

Journal: Bioorg Med Chem Lett

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

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

Abstract: 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.

CiteXplore: 18635349

DOI: 10.1016/j.bmcl.2008.06.095