Table 1.
Entrya | Anti-proliferationb | Her2 ELISAc | Luc. Refoldingd | |
---|---|---|---|---|
MCF-7 | SkBr3 | SkBr3 | ||
1 | >100e | 42 ± 4 | 67 ± 8 | 13 ± 4 |
2 | 41 ± 12 | 55 ± 8 | 64 ± 15 | NI |
3 | >100 | >100 | >100 | NI |
4 | >100 | >100 | >100 | 15 ± 0.6 |
5 | >100 | >100 | >100 | 4.4 ± 1.5 |
6 | 4 ± 1 | 23 ± 0.5 | 33 ± 6 | 36 ± 2 |
7 | 44 ± 8 | 55 ± 1 | 61 ± 1 | 15 ± 0.6 |
8 | >100 | >100 | >100 | 55 ± 9 |
9 | 3.0 ± 0.8 | 2.4 ± 1.1 | 4.4 ± 2.1 | 16 ± 1 |
10 | >100 | >100 | >100 | 2.1 ± 0.2 |
11 | 25 ± 11 | 9.0 ± 0.3 | 8.9 ± 3.4 | 7.0 ± 0.4 |
12 | 19 ± 4 | 7.8 ± 0.3 | 4.7 ± 1.7 | 120 ± 8 |
13 | >100 | >100 | >100 | 22 ± 0.5 |
14 | 93 ± 7 | 76 ± 12 | 44 ± 4.5 | 23 ± 8 |
15 | 2.1 ± 0.8 | 15 ± 1 | 12.5 ± 3.6 | 1.9 ± 0.3 |
16 | 9.1 ± 4 | 15 ± 6.2 | 10.9 ± 0.4 | 6.7 ± 2 |
17 | >100 | 25 ± 3.6 | 21.3 ± 14 | 15 ± 12 |
18 | >100 | >100 | >100 | 190 ± 4 |
19 | 34 ± 13 | 39 ± 2.1 | 51.6 ± 7 | 4.5 ± 0.3 |
20 | >100 | >100 | >100 | 0.12 ± 0.6 |
Compounds correspond to scaffolds shown in Figure 5.
Anti-proliferation assays were performed as described in Section 5.8.
Her2 ELISA assays were performed as described in Section 5.9.
Luciferase refolding assays were performed as described in Section 5.7.
Values represent Mean IC50 ± SE of at least two separate experiments performed in triplicate (μM).