Source:http://linkedlifedata.com/resource/pubmed/id/11392543
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
10
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pubmed:dateCreated |
2001-6-5
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pubmed:abstractText |
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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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0960-894X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
21
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pubmed:volume |
11
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1307-11
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:11392543-Animals,
pubmed-meshheading:11392543-Benzoic Acids,
pubmed-meshheading:11392543-Boranes,
pubmed-meshheading:11392543-Boron Neutron Capture Therapy,
pubmed-meshheading:11392543-COS Cells,
pubmed-meshheading:11392543-Cell Differentiation,
pubmed-meshheading:11392543-Dose-Response Relationship, Drug,
pubmed-meshheading:11392543-HL-60 Cells,
pubmed-meshheading:11392543-Humans,
pubmed-meshheading:11392543-Models, Molecular,
pubmed-meshheading:11392543-Molecular Conformation,
pubmed-meshheading:11392543-Receptors, Retinoic Acid,
pubmed-meshheading:11392543-Retinoids,
pubmed-meshheading:11392543-Structure-Activity Relationship,
pubmed-meshheading:11392543-Transcriptional Activation
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pubmed:year |
2001
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pubmed:articleTitle |
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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pubmed:affiliation |
Graduate School of Pharmaceutical Sciences, University of Tokyo, Japan. yendo@mol.f.u-tokyo.ac.jp
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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