Table 2.
Gαq/11 inhibitory activity and antitumor activity of GQ236‒GQ267a.
| Compd. | R1 | R2 (∗) | IP1 inhibition at 10 μmol/L | Antiproliferation (IC50, μmol/L) |
|
|---|---|---|---|---|---|
| MP41 | 92.1 | ||||
| GQ236 |  |
 |
48.4 ± 2.4% | 10.1 ± 0.2 | 9.3 ± 0.5 |
| GQ237 |  |
 |
43.0 ± 3.3% | 4.0 ± 1.3 | 5.8 ± 0.1 |
| GQ238 |  |
 |
34.4 ± 1.7% | 6.2 ± 0.7 | 7.3 ± 0.7 |
| GQ239 |  |
 |
50.2 ± 5.2% | 6.0 ± 0.6 | 11.6 ± 0.6 |
| GQ240 |  |
 |
22.5 ± 4.2% | 7.4 ± 0.3 | 9.6 ± 0.6 |
| GQ241 |  |
 |
31.3 ± 9.0% | 5.9 ± 0.5 | 6.6 ± 0.2 |
| GQ242 |  |
 |
41.0 ± 6.0% | 5.0 ± 0.1 | 4.7 ± 0.4 |
| GQ243 |  |
 |
41.6 ± 5.8% | 5.7 ± 0.7 | 9.6 ± 0.7 |
| GQ244 |  |
 |
45.8 ± 10.5% | 5.6 ± 0.3 | 9.0 ± 1.3 |
| GQ245 |  |
 |
46.8 ± 8.6% | 5.0 ± 0.3 | 5.7 ± 0.1 |
| GQ246 |  |
 |
40.4 ± 7.0% | 14.9 ± 0.8 | 15.8 ± 1.0 |
| GQ247 |  |
 |
44.5 ± 3.4% | 5.6 ± 0.2 | 6.0 ± 0.3 |
| GQ248 |  |
 |
49.7 ± 9.5% | 7.9 ± 0.7 | 10.9 ± 0.5 |
| GQ249 |  |
 |
44.1 ± 3.0% | 5.8 ± 0.6 | 11.4 ± 0.3 |
| GQ250 |  |
 |
41.8 ± 2.7% | 6.9 ± 1.0 | 10.4 ± 0.2 |
| GQ251 |  |
 |
51.2 ± 4.9% | 7.4 ± 0.8 | 12.6 ± 0.7 |
| GQ252 |  |
 |
35.9 ± 7.3% | 5.2 ± 0.7 | 3.5 ± 0.3 |
| GQ253 |  |
 |
32.4 ± 1.0% | 9.2 ± 0.6 | 9.7 ± 0.4 |
| GQ254 |  |
 |
44.2 ± 0.3% | 8.0 ± 0.6 | 11.2 ± 0.7 |
| GQ255 |  |
 |
27.7 ± 6.7% | > 40 | > 40 |
| GQ256 |  |
 |
47.6 ± 5.0% | 9.0 ± 1.2 | 8.7 ± 0.7 |
| GQ257 |  |
 |
33.2 ± 1.3% | 6.0 ± 0.3 | 9.6 ± 0.5 |
| GQ258 |  |
 |
48.3 ± 6.5% | 7.9 ± 1.5 | 11.6 ± 1.4 |
| GQ259 |  |
 |
36.3 ± 0.9% | 5.8 ± 0.6 | 10.7 ± 0.8 |
| GQ260 |  |
 |
53.4 ± 7.0% | 6.7 ± 0.6 | 11.6 ± 1.2 |
| GQ261 |  |
 |
27.0 ± 5.1% | 6.2 ± 0.8 | 11.0 ± 0.5 |
| GQ262 |  |
 |
57.2 ± 1.9% | 5.1 ± 0.6 | 10.4 ± 0.1 |
| GQ263 |  |
 |
38.9 ± 3.3% | 10.5 ± 0.7 | 11.0 ± 0.5 |
| GQ264 |  |
 |
5.9 ± 1.1% | > 40 | > 40 |
| GQ265 |  |
 |
13.5 ± 0.5% | > 40 | > 40 |
| GQ266 |  |
 |
17.5 ± 1.1% | > 40 | > 40 |
| GQ267 |  |
 |
8.9 ± 0.8% | > 40 | > 40 |
| 3 | 26.9 ± 3.3% | 11.9 ± 1.0 | 9.7 ± 0.1 | ||
a
IP1 accumulation assay was utilized to characterize Gαq/11 inhibitory activity. Antitumor activity was measured utilizing CCK-8 assay. Data represent the mean ± SEM (n = 3).