Title : Synthesis and CYP26A1 inhibitory activity of 1-[benzofuran-2-yl-(4-alkyl/aryl-phenyl)-methyl]-1H-triazoles.

Pub. Date : 2006 Jun 1

PMID : 16458519






5 Functional Relationships(s)
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1 Synthesis and CYP26A1 inhibitory activity of 1-[benzofuran-2-yl-(4-alkyl/aryl-phenyl)-methyl]-1H-triazoles. 1-[benzofuran-2-yl-(4-alkyl/aryl-phenyl)-methyl]-1h-triazoles cytochrome P450 family 26 subfamily A member 1 Homo sapiens
2 All the triazole derivatives were evaluated for CYP26A1 inhibitory activity using a MCF-7 cell-based assay. Triazoles cytochrome P450 family 26 subfamily A member 1 Homo sapiens
3 The 4-ethyl and 4-phenyl-1,2,4-triazole derivatives displayed inhibitory activity (IC(50) 4.5 and 7 microM, respectively) comparable with that of the CYP26 inhibitor liarozole (IC(50) 7 microM). liarozole cytochrome P450 family 26 subfamily A member 1 Homo sapiens
4 Using a CYP26A1 homology model (based on CYP3A4) template, docking experiments were performed with MOE with multiple hydrophobic interactions observed in addition to coordination between the triazole nitrogen and the haem transition metal. Triazoles cytochrome P450 family 26 subfamily A member 1 Homo sapiens
5 Using a CYP26A1 homology model (based on CYP3A4) template, docking experiments were performed with MOE with multiple hydrophobic interactions observed in addition to coordination between the triazole nitrogen and the haem transition metal. Nitrogen cytochrome P450 family 26 subfamily A member 1 Homo sapiens