Structure-Activity study of retinoid agonists bearing substituted dicarba-closo-dodecaborane. Relation between retinoidal activity and conformation of two aromatic nuclei.
Bioorg Med Chem Lett
; 11(10): 1307-11, 2001 May 21.
Article
em En
| MEDLINE
| ID: mdl-11392543
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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Base de dados:
MEDLINE
Assunto principal:
Retinoides
/
Boranos
Idioma:
En
Ano de publicação:
2001
Tipo de documento:
Article