Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
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Diarylamines Incorporating Hexahydrophenalene or Octahydrobenzoheptalene as Retinoid X Receptor (RXR)-Specific Agonists
Yohei Amano , Masayuki Noguchi, Koichi Shudo
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2014 Volume 62 Issue 3 Pages 254-259

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Abstract
Selective ligands for retinoic acid receptors (RARs) and for retinoid X receptors (RXRs) are required for both biological studies and therapeutic purposes. We have synthesized a series of diarylamines incorporating hexahydrophenalene or octahydrobenzoheptalene as a hydrophobic moiety and examined their activities towards RARs and RXRs. Most of these compounds showed agonistic activity towards RXRs, but were inactive towards RARs. These RXR-specific ligands showed synergistic activity in RARα,β ligand-induced terminal differentiation of leukemia cell line HL-60.
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© 2014 The Pharmaceutical Society of Japan
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