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. Author manuscript; available in PMC: 2019 May 10.
Published in final edited form as: Eur J Med Chem. 2018 Apr 12;151:777–796. doi: 10.1016/j.ejmech.2018.04.024

Table 1.

The inhibitory activity of compounds 1–6 against TDP2.

graphic file with name nihms961384u2.jpg
Cpd. X Y R IC50 (μM)a
TDP2 TDP2 WCE
1 N CH CO2Et 11 ± 1.0 22 ± 1.7
2 CH N CO2Et 43 ± 5.5 54 ± 2.5
3 N CH COMe 35 ± 5.1 36 ± 2.4
4 CH N COMe >111 NDb
5 N CH PO3Me2 >111 ND
6 CH N PO3Me2 99 ± 11 ND
a

The IC50 was expressed as mean ± SD from at least three independent experiments unless otherwise indicated.

b

“ND” means “not determined”.