Fig. 2. Structure-activity relationship of azole fungicides inhibiting 11β-HSDs.

11β-HSD1-dependent reduction of cortisone (200 nM) to cortisol and 11β-HSD2-dependent oxidation of cortisol (200 nM) to cortisone were measured using HEK-293 cell lysates in the presence of 500 μM NADPH or NAD⁺, respectively. Residual enzyme activity upon exposure to 20 μM test substance (mean ± SD) and IC₅₀ values (mean ± SD) were obtained from three independent experiments. For compounds with residual enzyme activities (% of control) >40%, at a compound concentration of 20 μM, IC₅₀ values were not determined (n.d.). a, values reported earlier by Vuorinen et al. [39].