Table 3.
In vitro inhibition of enzyme activities by the test compounds.
Arom |
STS |
17β-HSD1 |
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Comp. | Structure | Rel.conv. ± SD (%) | IC50 ± SD (µM) | Rel.conv. ± SD (%) | IC50 ± SD (µM) | Rel.conv. ± SD (%) | IC50 ± SD (µM) |
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6a | ![]() |
62 ± 1 | 64 ± 3 | 0.064 ± 0.034 | |||
7a | ![]() |
88 ± 2 | 0.23 ± 0.09 Ki = 0.36 ± 0.05 μM |
0.36 ± 0.25 | |||
8a | ![]() |
86 ± 6 | 80 ± 13 | 55 ± 7 | |||
6b | ![]() |
8.7 ± 2.8 | 2.0 ± 0.4 | 0.095 ± 0.031 | |||
7b | ![]() |
91 ± 6 | 0.89 ± 0.3 | 0.30 ± 0.20 | |||
8b | ![]() |
81 ± 5 | 2.1 ± 0.6 | 0.96 ± 0.45 | |||
6c | ![]() |
6.0 ± 1.2 | 2.4 ± 0.4 | 0.18 ± 0.02 | |||
7c | ![]() |
92 ± 3 | 1.6 ± 0.3 | 0.60 ± 0.16 | |||
8c | ![]() |
82 ± 4 | 3.0 ± 0.9 | 0.59 ± 0.16 | |||
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9 | ![]() |
85 ± 13 | 96 ± 1 | 1.2 ± 0.2 [12] Ki = 1.9 ± 0.2 μM |
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10a | ![]() |
82 ± 10 | 83 ± 3 | 0.59 ± 0.23 [13] | |||
11a | ![]() |
90 ± 7 | 6.0 ± 1.6 | 1.0 ± 0.3 [13] Ki = 2.2 ± 0.3 μM |
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12a | ![]() |
91 ± 1 | 2.4 ± 0.5 | 0.38 ± 0.08 [13] Ki= 0.94 ± 0.15 μM |
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10b | ![]() |
100 ± 5 | 81 ± 6 | 1.2 ± 0.3 [13] | |||
11b | ![]() |
78 ± 1 | 8.5 ± 3.1 | 2.1 ± 1.2 [13] | |||
12b | ![]() |
108 ± 11 | 71 ± 4 | 2.7 ± 0.1 [13] | |||
10c | ![]() |
106 ± 6 | 57 ± 1 | 0.33 ± 0.10 | |||
11c | ![]() |
98 ± 3 | 80 ± 7 | 2.6 ± 1.0 | |||
12c | ![]() |
101 ± 4 | 70 ± 3 | 2.2 ± 0.6 | |||
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13 | ![]() |
95 ± 12 | 76 ± 5 | 1.1 ± 0.33 Ki = 2.0 ± 0.4μM |
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14a | ![]() |
89 ± 9 | 3.9 ± 1.6 | 2.9 ± 1.6 | |||
15a | ![]() |
92 ± 7 | 2.7 ± 1.3 | 57 ± 9 | |||
16a | ![]() |
94 ± 2 | 59 ± 13 | 61 ± 7 | |||
14b | ![]() |
97 ± 5 | 4.1 ± 1.3 | 1.3 ± 0.8 | |||
15b | ![]() |
90 ± 8 | 3.7 ± 1.2 | 49 ± 12 | 11 ± 4 | ||
16b | ![]() |
82 ± 6 | 7.5 ± 2.0 | 4.1 ± 2.5 | |||
14c | ![]() |
88 ± 10 | 7.0 ± 1.9 | 2.6 ± 1.3 | |||
15c | ![]() |
89 ± 1 | 6.3 ± 1.8 | 4.5 ± 2.0 | |||
16c | ![]() |
82 ± 12 | 1.3 ± 0.4 Ki = 1.9 ± 0.2 μM | 53 ± 2 |