Literature DB >> 18054230

(2S,2'R)-analogue of LG190178 is a major active isomer.

Wataru Hakamata1, Yukiko Sato, Haruhiro Okuda, Shinobu Honzawa, Nozomi Saito, Seishi Kishimoto, Atsushi Yamashita, Takayuki Sugiura, Atsushi Kittaka, Masaaki Kurihara.   

Abstract

Vitamin D receptor (VDR) ligands are therapeutic agents for the treatment of psoriasis, osteoporosis, and secondary hyperparathyroidism. VDR ligands also show immense potential as therapeutic agents for autoimmune diseases and cancers of the skin, prostate, colon, and breast as well as leukemia. LG190178 is a novel non-secosteroidal ligand for VDR. We synthesized and evaluated stereoisomers of LG190178 and found that only an (2S,2'R)-analogue of LG190178 (YR301) had strong activity.

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Year:  2007        PMID: 18054230     DOI: 10.1016/j.bmcl.2007.11.007

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


  2 in total

1.  Structure of the ligand-binding domain of rat VDR in complex with the nonsecosteroidal vitamin D3 analogue YR301.

Authors:  Shinji Kakuda; Kazuhisa Okada; Hiroshi Eguchi; Kazuya Takenouchi; Wataru Hakamata; Masaaki Kurihara; Midori Takimoto-Kamimura
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2008-10-31

2.  Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold.

Authors:  Kelly A Teske; Ganesha Rai; Premchendar Nandhikonda; Preetpal S Sidhu; Belaynesh Feleke; Anton Simeonov; Adam Yasgar; Ajit Jadhav; David J Maloney; Leggy A Arnold
Journal:  ACS Comb Sci       Date:  2017-09-05       Impact factor: 3.903

  2 in total

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