Table 6.
Antiproliferative activities of the synthesized 7-deazapurines
| 7-deazapurine | cell viabilitya GI50, μM
|
|
|---|---|---|
| HeLa | MCF-7 | |
| rigidin A | > 100 | > 100 |
| rigidin B | > 100 | > 100 |
| rigidin C | > 100 | > 100 |
| rigidin D | > 100 | > 100 |
| 22e | > 100 | > 100 |
| 22f | > 100 | > 100 |
| 22g | > 100 | > 100 |
| 22h | > 100 | > 100 |
| 22i | 80 ± 10 | 14 ± 1 |
| 22j | 71 ± 12 | 47 ± 5 |
| 22k | > 100 | > 100 |
| 23a | > 100 | > 100 |
| 23b | > 100 | > 100 |
| 23c | 4.4 ± 0.4 | 3.9 ± 0.5 |
| 23d | 28 ± 4 | 15 ± 0 |
| 23e | > 100 | > 100 |
| 23f | > 100 | > 100 |
| 24a | 20 ± 1 | 8.0 ± 1 |
| 24b | 70 ± 15 | 75 ± 11 |
| 24c | 9.0 ± 1 | 7.0 ± 1 |
| 24d | 18 ± 10 | 10 ± 2 |
| 24e | 45 ± 9 | 51 ± 2 |
| 25a | 0.035 ± 0.007 | 0.040 ± 0.024 |
| 25b | 0.2 ± 0.1 | 0.150 ± 0.060 |
| 25c | 0.10 ± 0.07 | 0.06 ± 0.02 |
| 25d | 0.13 ± 0.05 | 0.06 ± 0.02 |
| 25e | 0.065 ± 0.010 | 0.070 ± 0.025 |
| 25f | 0.15 ± 0.05 | 0.135 ± 0.075 |
| 25g | 0.080 ± 0.025 | 0.087 ± 0.020 |
| 25h | 0.88 ± 0.06 | 1.26 ± 0.18 |
| 25i | 48 ± 8 | 33 ± 4 |
| 25j | 8.2 ± 1 | 40 ± 4 |
| 25k | 7.1 ± 1 | 10 ± 5 |
| 25l | 4.9 ± 0.3 | 2.2 ± 0.1 |
| 25m | 0.095 ± 0.040 | 0.095 ± 0.010 |
| 25n | 0.86 ± 0.06 | 1.09 ± 0.12 |
| 25o | 0.19 ± 0.01 | 0.25 ± 0.02 |
| 25p | 6.3 ± 1 | 0.80 ± 0.01 |
| 25q | >100 | 7.0 ± 1 |
| 25r | 0.30 ± 0.07 | 0.11 ± 0.035 |
| 25s | 0.40 ± 0.01 | 0.31 ± 0.01 |
| 25t | 2.2 ± 1 | 0.6 ± 0.1 |
| 25u | 0.045 ± 0.004 | 0.053 ± 0.005 |
| 25v | 43 ± 6 | 56 ± 2 |
| 25w | 0.4 ± 0.1 | 0.3 ± 0.07 |
| 25x | 0.30 ± 0.01 | 0.26 ± 0.05 |
| 25y | 5.0 ± 0.6 | 3.0 ± 0.6 |
| 25z | 4.0 ± 0.6 | 2.8 ± 0.8 |
a
Concentration required to reduce the viability of cells by 50% after a 48 h treatment with the indicated compounds relative to a DMSO control ± SD from two independent experiments, each performed in 4 replicates, as determined by the MTT assay.