Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton. Issue 22 (15th November 2015)

• Record Type: Journal Article
• Authors: Misawa, Takashi; Yorioka, Momoko; Demizu, Yosuke; Noguchi-Yachide, Tomomi; Ohoka, Nobumichi; Kurashima-Kinoshita, Megumi; Motoyoshi, Hitomi; Nojiri, Hisao; Kittaka, Atsushi; Makishima, Makoto; Naito, Mikihiko; Kurihara, Masaaki
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 22(2015)
• Page Start: 5362
• Page End: 5366
• Publication Date: 2015-11-15
• Subjects: Vitamin D receptor -- Non-secosteroidal VDR ligands -- Long alkyl chain; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.09.030
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Vitamin D receptor (VDR) is a family of nuclear receptors (NR) that regulates physiological effects such as the immune system, calcium homeostasis, and cell proliferation. We synthesized non-secosteroidal VDR ligands bearing a long alkyl chain based on the diphenylpentane skeleton. The VDR-mediated transcriptional activities of the synthesized compounds were evaluated using a reporter gene assay and HL-60 cell differentiation-inducing assay. We herein described the structure–activity relationship and effects of alkyl-chain length on VDR-mediated transcriptional activity.