Structure-activity study of estrogenic agonists bearing dicarba-closo-dodecaborane. Effect of geometry and separation distance of hydroxyl groups at the ends of molecules
Y. Endo et al., Structure-activity study of estrogenic agonists bearing dicarba-closo-dodecaborane. Effect of geometry and separation distance of hydroxyl groups at the ends of molecules, BIOORG MED, 9(23), 1999, pp. 3313-3318
Dicarba-closo-dodecaboranes (carboranes), which have spherical geometry and
hydrophobicity, are applicable as a hydrophobic pharmacophore of biologica
lly active molecules. We have investigated structure-activity relations bas
ed on the structure of the potent estrogenic agonist, 1-hydroxymethyl-12-(4
-hydroxyphenyl)-1,12-dicarba-closo-dodecaborane, which we have previously r
eported. The geometry and separation distance of the phenolic and alcoholic
hydroxyl groups play a critical role in the appearance of biological activ
ity. (C) 1999 Elsevier Science Ltd. All rights reserved.