Table 3.
Compound # |
X | R | secretion IC50 (µM) |
translocation IC50 (µM) |
translocation CC50 (µM) |
---|---|---|---|---|---|
1 | O | 3,4-methylenedioxy | 7.8 ± 2.0 | 11 ± 2 | >100 |
2 | O | 4-F | 9.8 ± 2.9 | 6.7 ± 1.0 | 59 ± 16 |
20a | S | 3,4-methylenedioxy | 7.8 ± 2.0 | >100 | >100 |
20b | S | 4-F | 7.8 ± 2.0 | >100 | >100 |
21a | SO2 | 3,4-methylenedioxy | >100 | n.d. | n.d. |
21b | SO2 | 4-F | >100 | n.d. | n.d. |
23a | NH | 3,4-methylenedioxy | 45 ± 4 | >100 | >100 |
23b | NH | 4-F | 34 ± 8 | 32 ± 5 | >100 |
25a | CH2 | 3,4-methylenedioxy | >100 | n.d. | n.d. |
25b | CH2 | 4-F | >100 | n.d. | n.d. |
n.d.: value not determined