Table 1.
Biological evaluation of 1, 2, and 3.
| PKC affinity | cellular growth inhibition | ||
|---|---|---|---|
| Ki (nM)a | A549 EC50 (nM)b | K562 EC50 (nM)b | |
| 1c | 0.48 ± 0.07 | 150 ± 30 | 7 ± 1 |
| 2 | 343 ± 6 | >10,000 | >10,000 |
| 3 | 1.6 ± 0.1 | 1500 ± 60 | 87 ± 5 |
Ki values determined in duplicate experiments.
EC50 values determined in triplicate experiments. All errors shown are standard errors of the mean.
A sample of yuanhuapin 1 was provided by Prof. Yue, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, China.