Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton.
Basic Information
ID: ALA3632608
Journal: Bioorg Med Chem Lett
Title: Effects of alkyl side chains and terminal hydrophilicity on vitamin D receptor (VDR) agonistic activity based on the diphenylpentane skeleton.
Authors: Misawa T, Yorioka M, Demizu Y, Noguchi-Yachide T, Ohoka N, Kurashima-Kinoshita M, Motoyoshi H, Nojiri H, Kittaka A, Makishima M, Naito M, Kurihara M.
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.
CiteXplore: 26432035
DOI: 10.1016/j.bmcl.2015.09.030
Patent ID: ┄