TABLE 2.
In vitro cytotoxicities of sipanmycins and derivatives
| Sipanmycin or derivative | Cytotoxicity (IC50 [μM]) by cell type (source) |
|||||
|---|---|---|---|---|---|---|
| 3T3 (fibroblasts) | A549 (lung) | HT29 (colon) | HL60 (leukemia) | CAPAN-1 (pancreas) | MDAMB231 (breast) | |
| Sipanmycin A | 0.302 | 0.117 | 0.189 | 0.796 | 0.178 | 0.095 |
| Sipanmycin B | 0.411 | 0.118 | 0.264 | 1.52 | 0.747 | 0.188 |
| AgA (compound 1) | ≫10 | ≫10 | ≫10 | 2.549 | ≫10 | ≫10 |
| AgB (compound 2) | ≫10 | >10 | >10 | 0.698 | ≫10 | >10 |
| AgA+S1 (compound 3) | 0.91 | 0.647 | 0.431 | 1.16 | 2.17 | 0.827 |
| dOHSipA (compound 5) | 1.614 | 1.75 | 0.873 | 1.089 | 2.68 | 1.2 |
| dSipA (compound 6) | 0.163 | 0.147 | 0.147 | 0.468 | 0.181 | 0.085 |
| dSipB (compound 7) | 0.293 | 0.211 | 0.213 | 1.129 | 0.493 | 0.241 |