Literature DB >> 18635349

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

Kaori Cho1, Fumito Uneuchi, Yuko Kato-Nakamura, Jun-ichi Namekawa, Seiichi Ishizuka, Kazuya Takenouchi, Kazuo Nagasawa.   

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.

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Year:  2008        PMID： 18635349     DOI： 10.1016/j.bmcl.2008.06.095

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

1.  Discovery of the first irreversible small molecule inhibitors of the interaction between the vitamin D receptor and coactivators.

Authors:  Premchendar Nandhikonda; Wen Z Lynt; Megan M McCallum; Tahniyath Ara; Athena M Baranowski; Nina Y Yuan; Dana Pearson; Daniel D Bikle; R Kiplin Guy; Leggy A Arnold
Journal:  J Med Chem       Date:  2012-05-16       Impact factor: 7.446

Review 2.  Inhibitors for the Vitamin D Receptor-Coregulator Interaction.

Authors:  Kelly A Teske; Olivia Yu; Leggy A Arnold
Journal:  Vitam Horm       Date:  2015-11-30       Impact factor: 3.421

3.  Peroxisome proliferation-activated receptor δ agonist GW0742 interacts weakly with multiple nuclear receptors, including the vitamin D receptor.

Authors:  Premchendar Nandhikonda; Adam Yasgar; Athena M Baranowski; Preetpal S Sidhu; Megan M McCallum; Alan J Pawlak; Kelly Teske; Belaynesh Feleke; Nina Y Yuan; Chinedum Kevin; Daniel D Bikle; Steven D Ayers; Paul Webb; Ganesha Rai; Anton Simeonov; Ajit Jadhav; David Maloney; Leggy A Arnold
Journal:  Biochemistry       Date:  2013-06-10       Impact factor: 3.321
  3 in total

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