Table 1.

TOP1 and TDP1 Inhibitions, Enhanced Melting Temperature with dsDNA and Cytotoxicity of the Indicated Compounds

^aTOP1 cleavage inhibitory activity of synthesized compounds was semiquantitatively expressed relative to CPT at 1 μM as follows: 0, no inhibition; +, between 20% and 50% activity; ++, between 50% and 75% activity; +++, between 75% and 95% activity; ++++, equal activity.

^bTDP1 inhibition was determined by using a fluorescence assay and the percentage inhibition of the compounds at 100 μM concentration was calculated. Every experiment was repeated at least three times independently.

^cΔT_m = T_m(DNA + compound) − T_m(DNA). Every experiment was repeated at least twice independently.

^dGI₅₀ values (means ± SD) were defined as the concentrations of compounds that resulted in 50% cell growth inhibition and obtained from MTT assay. Every experiment was repeated at least three times independently.

^e“/” mean “ inapplicable”.

^f“ND” mean ” not determined”.