Structure-Activity study of retinoid agonists bearing substituted dicarba-closo-dodecaborane. Relation between retinoidal activity and conformation of two aromatic nuclei |
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Authors: | Endo Y Iijima T Yaguchi K Kawachi E Inoue N Kagechika H Kubo A Itai A |
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Institution: | Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan. yendo@mol.f.u-tokyo.ac.jp |
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Abstract: | We have investigated the structure activity relationships of the potent retinoid agonist, 4-4-(2-propyl-1,2-dicarba-closo-dodecaboran-l-yl)phenylamino]benzoic acid (BR403), which we have previously reported. Substitution of a methyl group on the aromatic nucleus or a methyl group on the nitrogen atom, or replacement of the amino group with ether, methylene, carboxyl or 1,1-ethylene greatly decreased the activity. The relatively planar conformation at the phenyl-N-phenyl moiety seems to play a critical role in the appearance of the biological activity. |
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