Table 3. Selectivity of the Most Active 17β-HSD2 Inhibitors toward 17β-HSD1.
compound | 17β-HSD2 activity (IC50) | 17β-HSD1 activity (IC50 or remaining activity at 20 μM) | selectivity factor |
---|---|---|---|
nordihydroguaiaretic acid (1) | 0.38 ± 0.04 μM | 5.5 ± 1.3 μM | 15 |
curcumin (3) | 1.73 ± 0.20 μM | 52.2 ± 7.1% | ∼12 |
(−)-dihydroguaiaretic acid (4) | 0.94 ± 0.02 μM | 7.7 ± 2.2 μM | 8 |
isoliquiritigenin (6) | 0.36 ± 0.08 μM | 2.83 ± 0.80 μM | 8 |
lupinalbin A (8) | 1.52 ± 0.15 μM | 0.049 ± 0.019 μM | 0.03 |
2′-hydroxygenistein (9) | 2.03 ± 0.37 μM | 1.09 ± 0.06 μM | 0.5 |
rosmarinic acid (11) | 3.72 ± 0.17 μM | n.i.a | >5 |
ethyl vanillate (12) | 1.28 ± 0.26 μM | n.i. | >15 |
2-(3-chloro-4-hydroxyphenyl)-N-phenethylacetamide (13) | 1.57 ± 0.16 μM | n.i. | >12 |
N-benzyl-2-(3-chloro-4-hydroxyphenyl)acetamide (16) | 3.42 ± 0.74 μM | n.i. | >5 |
N-(2-(1H-indol-3-yl)ethyl)-2-(3-chloro-4-hydroxyphenyl)acetamide (17) | 0.98 ± 0.24 μM | n.i. | >20 |
2-(3-chloro-4-hydroxyphenyl)-N-(2-chlorobenzyl)acetamide (18) | 0.78 ± 0.16 μM | 54.8 ± 5.8% | ∼25 |
n.i., no inhibition.