Synthesis and characterization of azole isoflavone inhibitors of aromatase.
Article Details
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Hackett JC, Kim YW, Su B, Brueggemeier RW
Synthesis and characterization of azole isoflavone inhibitors of aromatase.
Bioorg Med Chem. 2005 Jun 2;13(12):4063-70. Epub 2005 Apr 25.
- PubMed ID
- 15911319 [ View in PubMed]
- Abstract
The synthesis and biological evaluation of a series of 2-azole and 2-thioazole isoflavones as potential aromatase inhibitors are described. Differences in inhibitory activity of triazole and imidazole inhibitors are rationalized with density functional theory to expose a key difference in the electronic structure of these molecules. In addition, difference binding spectra of inhibitors to immunoaffinity-purified aromatase produces classical Type II spectra consistent with coordination of the nitrogen lone pair electrons to the aromatase P450 heme.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Aminoglutethimide Cytochrome P450 19A1 Ki (nM) 1410 7 37 Details Aminoglutethimide Cytochrome P450 19A1 IC 50 (nM) 2800 7 37 Details