| |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Compound | 8a | 6t | 8b | 8c | 8d | 8e | 8f | 8g | 8h | 8i | 8j |
| R1 | CO2H | H | CO2H | CO2H | CO2H | CO2H | CO2H | CO2H | CO2H | H | CO2H |
| R2 | H | H | H | H | H | H | H | H | H | H | H |
| R3 | H | H | CH3 | OBn | CF3 | NO2 | OH | SO3H | CO2H | CO2H | H |
| R4 | H | H | H | H | H | H | H | H | H | H | CO2H |
| R5 | H | H | H | H | H | H | H | H | H | H | CO2H |
| X | CH | CH | CH | CH | CH | CH | CH | CH | CH | CH | CH |
| IC50a (μM) | 9.3 | >100 | 14.8 | 12.7 | 4.2 | 3.2 | >100 | >100 | >100 | 40.1 | >100 |
Half maximal inhibitory concentrations (IC50 values) obtained from in vitro TDP1 gel-based assays.