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. 2017 Mar 20;80(4):965–974. doi: 10.1021/acs.jnatprod.6b00950

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
a

n.i., no inhibition.