PubMed:10212389 JSONTXT

{"target":"https://pubannotation.org/docs/sourcedb/PubMed/sourceid/10212389","sourcedb":"PubMed","sourceid":"10212389","source_url":"http://www.ncbi.nlm.nih.gov/pubmed/10212389","text":"Dicarba-closo-dodecaboranes as a pharmacophore. Retinoidal antagonists and potential agonists.\nSynthesis and biological evaluation of the first dicarba-closo-dodecaborane (carborane) derivatives of retinoids are described. Their retinoidal activity were examined in terms of the differentiation-inducing ability toward human promyelocytic leukemia HL-60 cells. High retinoidal activity (agonist or antagonist for retinoic acid receptor (RAR) requires a carboxylic acid moiety and an appropriate hydrophobic group located at a suitable position on the molecule. The 4-carboranyl-substituted compounds (7, 11) showed antagonistic activity but no agonistic activity even in the presence of the potent synergist HX630. On the other hand, the 3-carboranyl-substituted compounds (8, 12) showed potential agonistic activity, but no antagonistic activity. The results indicates that carboranes are applicable as the hydrophobic moiety of biologically active 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