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IC50s for inhibition of topoisomerase activitiesa
| Compound | IC50 (μM) for enzyme: |
|||
|---|---|---|---|---|
| M. tuberculosis topoisomerase I | E. coli DNA gyrase | Human topoisomerase I | Human topoisomerase IIα | |
| 2471-12 | 7.5 | 160 | 80 | 80 |
| 2471-24 | 7.5 | >160 | >160 | 160 |
| 2471-36 | 15 | >160 | >160 | >160 |
| 2471-80 | 5 | 160 | 80 | 80 |
As an example, gel images of the topoisomerase inhibition assay for 2471-80 are shown in Fig. S2 in the supplemental material.
