Bioorganic & Medicinal Chemistry
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.
Hackett, John C.; Kim, Young Woo; Su, Bin; and Brueggemeier, Robert W., "Synthesis and Characterization of Azole Isoflavone Inhibitors of Aromatase" (2005). Chemistry Faculty Publications. 413.
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