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. Author manuscript; available in PMC: 2021 Apr 30.
Published in final edited form as: J Med Chem. 2018 Oct 31;61(22):9908–9930. doi: 10.1021/acs.jmedchem.8b00639

Table 4.

Cytotoxicity of the 19a in Drug-Resistant Isogenic Human Cancer Cell Lines

GI50 ± SD (μM)a
compd parental cell line resistant subline resistance ratiob
HCT116 HCT116-siTOP1
19a 0.076 ± 0.010 0.45 ± 0.31 5.9
1 0.009 ± 0.001 0.075 ± 0.014 8.3
DU-145 DU145-RC0.1
19a 0.018 ± 0.002 2.38 ± 0.34 132
1 0.021 ± 0.016 4.73 ± 0.68 225
MCF-7 MCF-7/ADR
19a 0.34 ± 0.098 0.95 ± 0.35 2.8
DOX 0.15 ± 0.003 11.67 ± 1.94 77.8
HepG2 HepG2/ADR
19a 0.30 ± 0.050 3.20 ± 0.40 10.7
DOX 0.19 ± 0.048 9.04 ± 0.14 47.6
a

GI50 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.

b

Resistance ratio was calculated by dividing the GI50 of the mutant cell line by the GI50 of the corresponding parental cell line.