Figure 9 | Scientific Reports

Figure 9

From: Identification of Leishmania donovani Topoisomerase 1 inhibitors via intuitive scaffold hopping and bioisosteric modification of known Top 1 inhibitors

Figure 9

(a) Simultaneous assay: Lane 1, 90 fmol of pBS(SK+) DNA; Lanes 2 → 4, same as lane 1, but incubated simultaneously with 30 fmol of LdTop1 with reaction buffer, 2% DMSO and camptothecin respectively, for 30 min at 37 °C; lanes 5–10, same as lane 1, but incubated simultaneously with 30 fmol of LdTop1 with the variable concentrations of compound 4 (as indicated) with pBS (SKþ) DNA at 37 °C for 30 min. The corresponding quantitative representation of percentage inhibition of LdTop1 under simultaneous conditions in the presence of indicated compound 4 concentrations in relaxation experiments; (b) Preincubation assay: Lane 1, 90 fmol of pBS(SK+) DNA; Lanes 2 → 4, same as lane 1, but DNA was added after preincubation with 30 fmol of LdTop1 with reaction buffer, 2% DMSO and with camptothecin, respectively, for 30 min at 37 °C; lanes 5–10, same as lane 1, but preincubation of LdTop1 with the variable concentrations of compound 4 (as indicated) with pBS (SKþ) DNA at 37 °C for 30 min. The corresponding quantitative representation of percentage inhibition of LdTop1 under preincubation conditions in the presence of indicated compound 4 concentrations in relaxation experiments. All the experiments were conducted thrice and representative data from once set of them are expressed as mean ± SD.

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