Chemical and Pharmaceutical Bulletin p. 398 - 404 (1999)
Update date:2022-08-24
Topics:
Iijima, Toru
Endo, Yasuyuki
Tsuji, Motonori
Kawachi, Emiko
Kagechika, Hiroyuki
Shudo, Koichi
Synthesis 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 molecules.
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