Table 1. Comparison of SM145 and Compounds 1–7.
| compound | IC50 HCT-116 (μM) | IC50 MiaPaCa-2 (μM) | % yield | ClogP | saturated solution of 80% EtOH/20% H2O |
|---|---|---|---|---|---|
| SM145 | 7.4 ± 0.5 | 7.8 ± 0.5 | 1–7% | 9.02 | 5.2 mg/mL |
| 1 | 7.6 ± 0.4 | 12.8 ± 2.3 | 40% | 9.09 | 2.1 mg/mL |
| 2 | 18.1 ± 0.4 | 23.6 ± 2.5 | 25% | 7.60 | N.D.a |
| 3 | 20.8 ± 2.5 | 23.0 ± 2.8 | 28% | 7.60 | N.D. |
| 4 | 15.7 ± 2.9 | 18.5 ± 5.3 | 30% | 7.60 | N.D. |
| 5 | 3.9 ± 0.2 | 4.5 ± 0.9 | 32% | 9.02 | 1.9 mg/mL |
| 6 | 5.1 ± 0.6 | 4.4 ± 0.7 | 30% | 9.09 | 1.5 mg/mL |
| 7 (SM253) | 5.0 ± 0.5 | 5.5 ± 0.2 | 40% | 7.44 | 9.5 mg/mL |
a
N.D.: not determined.