Table 1. hPXR-Binding Activities of Vinblastine (10), Its Fragments of Catharanthine (13) and Vindoline (14), and Their Relevant Analoguesa.
| inhibitory activity |
binding affinity | |||
|---|---|---|---|---|
| chemical | at 100 μM | IC50 | Ki | Kd |
| deacetyl vinblastine (12) | 40% | NA | NA | NT |
| vinblastine (10) | 60% | 71.4 μM | 62.2 μM | NT |
| BODIPY FL vinblastine (4) | NT | NA | NA | 297 nM |
| deacetyl vindoline (16) | 73% | 41.4 μM | 36.0 μM | NT |
| vindoline (14) | 93% | 12.9 μM | 11.2 μM | NT |
| BODIPY FL vindoline (20) | NT | NA | NA | 256 nM |
| sulfo-Cy5 vindoline (21) | NT | NA | NA | inactive |
| catharanthinic acid (15) | 44% | NA | NA | NT |
| catharanthine (13) | 73% | 20.5 μM | 17.8 μM | NT |
| BODIPY FL catharanthine (19) | NT | NA | NA | inactive |
a
Abbreviations: NA, not applicable; NT, not tested.