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  • Title: Dicarba-closo-dodecaboranes as a pharmacophore. Novel potent retinoidal agonists.
    Author: Endo Y, Iijima T, Kagechika H, Ohta K, Kawachi E, Shudo K.
    Journal: Chem Pharm Bull (Tokyo); 1999 Apr; 47(4):585-7. PubMed ID: 10319433.
    Abstract:
    The synthesis and biological evaluation of the dicarba-closo-dodecaborane (carborane) derivatives of retinoids are described. Retinoidal activity was examined in terms of the differentiation-inducing ability toward human promyelocytic leukemia HL-60 cells. High retinoidal activity (agonist or antagonist for the retinoid receptor RAR) requires a carboxylic acid moiety and an appropriate hydrophobic group located at a suitable position on the molecule. 4-[4-(1,2-Dicarba-closo-dodecaboran-1-yl)phenylamino]b enzoic acids and 4-[3-(1,2-dicarba-closo-dodecaboran-1-yl)phenylamino]b enzoic acids showed potent agonistic activity at concentrations of 10(-8)-10(-9) M. The results indicate that carboranes are applicable as the hydrophobic moiety of biologically active molecules.
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