Table 6.

TDP2 inhibitory activity, permeability and cytotoxicity profiles of selected analogues.

Compd	TDP2 IC50 (μM)a	PAMPA Pe (10−6 cm/s)b	CC50 (μM)c
			HepG2	HeLa
11a	0.20 ± 0.02	1.2	14	12
11e	0.15 ± 0.01	0.6	29	29
12a	0.033 ± 0.001	0.1	50	>100
12b	0.033 ± 0.002	0.08	41	45
12g	0.0073 ± 0.0003	0.04	85	65
12h	0.020 ± 0.002	0.07	82	90
12j	0.0065 ± 0.0004	0.02	>100	>100
12k	0.0061 ± 0.0006	0.06	>100	>100
4ad	0.041 ± 0.003	0.003	>100	>100
4bd	0.042 ± 0.004	0.01	>100	--
4cd	0.14 ± 0.01	0.008	>100	--

^aIC₅₀: concentration of a compound producing 50% inhibition, expressed as mean ± standard deviation from three independent experiments.

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

^cCC₅₀: concentration of a compound causing 50% cell death.

^dPreviously reported¹⁵ analogues.