Table 1. In vitro and cellular IC50 values of TDRL-505 and its analogs.
The in vitro IC50 values are based on EMSA reactions as described in Methods. RPA was incubated with the above compounds at concentration range of 1–125 μM. The cellular IC50 values are calculated from clonogenic survival assays as described in Methods. The cells were treated with the above compounds at a concentration range of 1–200 μM. Only four compounds were tested for cellular activity, the rest are indicated with ‘na’ meaning data not available since the experiments were not performed.
ENTRY | COMPOUND | Y | R | n | In vitro IC50 (μM) | Cellular IC50 (μM) |
---|---|---|---|---|---|---|
1 | TDRL-505 | p-Br | Et | 1 | 38 | >50 |
2 | TDRL-533 | p-Br | Me | 1 | >50 | >50 |
3 | TDRL-540 | p-F | Me | 1 | >100 | na |
4 | TDRL-543 | p-Br | Et | 2 | 25 | 50 |
5 | TDRL-539 | p-F | Me | 2 | >100 | na |
6 | TDRL-534 | p-Br | Me | 2 | 35 | na |
7 | TDRL-556 | p-Br | iPr | 2 | 43 | na |
8 | TDRL-551 | p-I | Et | 2 | 18 | 25 |
9 | TDRL-557 | p-F3CO | Et | 2 | 30 | na |
10 | TDRL-652 | m-I | Et | 2 | 15 | na |
11 | TDRL-617 | See below | >100 | na | ||
12 | TDRL-634 | See below | >100 | na | ||
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