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. Author manuscript; available in PMC: 2021 Feb 12.
Published in final edited form as: J Med Chem. 2020 Oct 20;63(21):12873–12886. doi: 10.1021/acs.jmedchem.0c00774

Figure 3.

Figure 3.

Compound 14 does not intercalate into DNA in the concentration range in which it inhibits topoIIα. A topoisomerase I-DNA unwinding assay was used to monitor intercalation. An ethidium bromide-strained agarose gel is shown. A relaxed DNA control (DNA) is included. The positions of nicked and supercoiled DNA are indicated. Relaxed DNA bands display an electrophoretic mobility between the nicked (more relaxed) and supercoiled (less relaxed) bands. Intercalation is indicated by the shift in the position of the plasmid from relaxed to negatively supercoiled. The effects of 10 µM ethidium bromide (EtBr, a strong intercalator) and 100 µM etoposide (a non-intercalator) on the DNA unwinding assay are shown as controls. The gel is representative of at least three independent experiments.