Novel Tetralone-Derived Retinoic Acid Metabolism Blocking Agents: Synthesis and in Vitro Evaluation with Liver Microsomal and MCF-7 CYP26A1 Cell Assays

The potent inhibitory activity of novel 2-benzyltetralone and 2-benzylidenetetralone derivatives vs liver microsomal retinoic acid metabolizing enzymes and a MCF-7 CYP26A1 cell assay is described. In the liver microsomal assay, the 2-biphenylmethyl-6-hydroxytetralone derivatives 16a and 16b were fou...

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Veröffentlicht in:	Journal of medicinal chemistry 2005-11, Vol.48 (23), p.7123-7131
Hauptverfasser:	Yee, Sook Wah, Jarno, Laetitia, Gomaa, Mohamed Sayed, Elford, Carole, Ooi, Li-Ling, Coogan, Michael P, McClelland, Richard, Nicholson, Robert Ian, Evans, Bronwen A. J, Brancale, Andrea, Simons, Claire
Format:	Artikel
Sprache:	eng
Schlagworte:	Binding Sites Biological and medical sciences Cell Line, Tumor Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Enzyme System - biosynthesis Humans In Vitro Techniques Medical sciences Microsomes, Liver - drug effects Microsomes, Liver - metabolism Miscellaneous Models, Biological Models, Molecular Pharmacology. Drug treatments Retinoic Acid 4-Hydroxylase Stereoisomerism Structure-Activity Relationship Tetralones - chemical synthesis Tetralones - chemistry Tetralones - pharmacology Tretinoin - antagonists & inhibitors Tretinoin - metabolism
Online-Zugang:	Volltext
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