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. Author manuscript; available in PMC: 2019 Oct 11.
Published in final edited form as: J Med Chem. 2018 Sep 27;61(19):8613–8624. doi: 10.1021/acs.jmedchem.8b00498

Table 1.

Anticancer activity of hexacyclic CPTs against eleven human cancer cell lines.

Cell line Compound IC50 (μM) a
Topotecan 1 2 3 4 5 6 7 8 9 10 11
A549 1.424 1.028 2.057 2.169 1.394 1.124 3.371 1.502 0.092 0.170 1.832 6.472
MCF-7 2.135 1.157 2.314 10.846 4.640 2.135 7.865 6.438 > 10 > 10 > 10 > 10
MDA-MB-231 1.898 0.488 1.542 1.323 1.439 0.562 2.135 1.996 0.348 0.425 0.641 5.016
HepG-2 0.237 0.064 0.180 1.106 0.016 0.063 0.079 0.071 0.055 0.060 0.348 0.971
KB 2.610 3.342 2.571 9.761 2.204 2.247 2.202 2.039 0.916 0.935 7.143 7.282
BEL-7402 7.118 10.54 2.442 > 10 3.480 2.022 2.135 1.931 0.275 0.425 2.015 > 10
SMMC-7721 11.627 > 10 3.085 > 10 10.441 > 10 11.011 > 10 > 10 8.503 > 10 > 10
MGC80-3 0.190 0.514 0.231 0.390 0.018 0.085 0.090 0.054 0.064 0.062 0.275 0.971
SK-N-SH 0.093 0.463 NT b 0.325 NT b NT b NT b NT b 0.348 0.51 0.549 0.194
QGY-7703 11.864 > 10 11.568 > 10 11.601 > 10 > 10 > 10 > 10 > 10 > 10 > 10
SGC-7901 > 10 > 10 > 10 > 10 > 10 > 10 > 10 > 10 > 10 > 10 > 10 > 10
a

Values are the mean of at least three data points.

b

Not Tested.