Table 1. In vitro and cellular IC50 values of TDRL-505 and its analogs.
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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