Table 6.
Compound # |
Ar | secretion IC50 (µM) |
translocation IC50 (µM) |
translocation CC50 (µM) |
---|---|---|---|---|
1 | 3,4-methylenedioxyphenyl | 7.8 ± 2.0 | 11.1 ± 2.3 | >100 |
2 | 4-fluorophenyl | 9.8 ± 2.9 | 6.7 ± 1.0 | 59 ± 16 |
34a | phenyl | 11 ± 3 | 12 ± 7 | 95 ± 21 |
34b | 3-fluorophenyl | 15 ± 3 | >27 | 27 ± 1 |
34c | 2-fluorophenyl | 6.3 ± 1.4 | 8.3 ± 3.0 | 47± 2 |
34d | 4-chlorophenyl | 8.5 ± 2.6 | >39 | 39 ± 8 |
34e | 3-chlorophenyl | 9.6 ± 4.1 | >19 | 19 ± 10 |
34f | 2-chlorophenyl | 9.2 ± 2.6 | 9.7 ± 4.2 | >100 |
34g | 4-methylphenyl | 8.1 ± 1.8 | >25 | 25 ± 7 |
34h | 3-methylphenyl | 8.5 ± 0.1 | >45 | 45 ± 7 |
34i | 2-methylphenyl | 11 ± 1 | >100 | >100 |
34j | 4-methoxyphenyl | 12 ± 5 | 23 ± 10 | 71 ± 2 |
34k | 3-methoxyphenyl | 16 ± 7 | >100 | >100 |
34l | 2-methoxyphenyl | 28 ± 5 | n.d. | n.d. |
34m | 3,4-dimethoxyphenyl | 22 ± 2 | >36 | 36 ± 6 |
34n | 2,4-dimethoxyphenyl | 19 ± 4 | >100 | >100 |
34o | benzothiophene-5-yl | 6.0 ± 1.6 | 5.3 ± 3.7 | 30 ± 11 |
34p | benzofuran-5-yl | 3.7 ± 1.6 | >11 | 11 ± 5 |
34q | benzimidazole-5-yl | 11 ± 5 | 33 ± 8 | 62 ± 7 |
34r | indole-5-yl | 2.1 ± 0.6 | 4.8 ± 0.4 | >100 |
34s | indole-6-yl | 1.9 ± 0.3 | 5.7 ± 0.6 | 9.4 ± 3.6 |
34t | indole-4-yl | 4.8 ± 1.2 | 4.3 ± 2.3 | 24 ± 2 |
34u | indole-2-yl | 8.9 ± 0.2 | >12 | 12 ± 4 |
34v | 1-methylindole-5-yl | 5.1 ± 1.4 | >6.3 | 6.3 ± 2.6 |
34w | pyrrolo[2,3-b]pyridin-5-yl | 9.5 ± 1.3 | >21 | 21 ± 4 |
34x | 6-fluoropyridin-3-yl | 58 ± 20 | >100 | >100 |
34y | 5-fluoropyridin-2-yl | 41 ± 18 | >100 | >100 |
n.d.: value not determined