Title of article
Novel retinoid X receptor (RXR) antagonists having a dicarba-closo-dodecaborane as a hydrophobic moiety
Author/Authors
Kiminori Ohta، نويسنده , , Toru Iijima، نويسنده , , Emiko Kawachi، نويسنده , , Hiroyuki Kagechika، نويسنده , , Yasuyuki Endo، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
6
From page
5913
To page
5918
Abstract
We designed and synthesized novel retinoid X receptor (RXR)-selective antagonists bearing a carborane moiety. Compounds 8a–d or 9a–d themselves have no differentiation-inducing activity toward HL-60 cells and no inhibitory activity towards a retinoic acid receptor (RAR) agonist. However, they inhibit the synergistic activity of an RXR agonist, PA024, in the presence of Am80 on the cell differentiation of HL-60. Transactivation assay using RARs and RXRs suggested that the inhibitory activity of 9b resulted from the selective antagonism at the RXR site of RXR–RAR heterodimers.
Keywords
retinoid X receptor , Antagonist , Carborane , Hydrophobicinteraction.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795095
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