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. Author manuscript; available in PMC: 2020 May 9.
Published in final edited form as: J Med Chem. 2019 Apr 30;62(9):4669–4682. doi: 10.1021/acs.jmedchem.9b00274

Table 4.

TDP2 inhibitory activity and PAMPA permeability for additional analogues of subtype 12 with N-10 phenyl A modifications.

graphic file with name nihms-1024966-t0008.jpg
Compd R TDP2 IC50 (μM)a PAMPA Pe (10−6 cm/s)b
12b 4′ OH 0.033 ± 0.002 0.08
12j 4′ NHSO2Me 0.0065 ± 0.0004 0.02
12g 3′ OH 0.0073 ± 0.0003 0.04
12k 3′ NHSO2Me 0.0061 ± 0.0006 0.06
12l H 0.27 ± 0.02 4.4
a

IC50: concentration of a compound producing 50% inhibition, expressed as mean ± standard deviation from three independent experiments performed in triplicate.

b

Pe: effective permeability coefficients determined using the PAMPA, measured in five replicates.