Table 2.

The structures and inhibitory activity of compounds 8–55 against TDP2.

Cpd.	R	IC50 (μM)a		Cpd.	R	IC50 (μM)a
		TDP2	TDP2 WCE			TDP2	TDP2 WCE
8	NHEt	>111	NDb	32	3-OC6H4Cl	14 ± 1.8	11 ± 1.1
9	NHPh	>111	ND	33	4-OC6H4Cl	11 ± 1.4	7.5 ± 0.56
10	2-NHC6H4OH	>111	ND	34	2-OC6H4CN	>111	>111
11	4-NHC6H4OMe	>111	ND	35	3-OC6H4CN	12 ± 1.8	10 ± 2.7
12	3-NHC6H4Cl	>111	ND	36	4-OC6H4CN	15 ± 2.1	13 ± 4.5
13	OMe	26 ± 3.3	12 ± 1.1	37	4-OC6H4Br	35 ± 4.8	12 ± 0.92
14	OCH2CF3	28 ± 11	24 ± 6.8	38	4-OC6H4SO2Me	14 ± 2.1	16 ± 4.2
15	OCH2CO2H	51 ± 20	37 ± 6.4	39	4-OC6H4NO2	28 ± 5.7	ND
16	O(CH2)2OH	20 ± 1.3	9.8 ± 1.4	40	2-OC10H7	>111	ND
17	O(CH2)3OH	17 ± 2.2	11 ± 0.62	41	3-pyridinyloxy	8.8 ± 1.1	7.7 ± 0.61
18	O(CH2)4OH	26 ± 4.2	12 ± 0.36	42		71 ± 54	ND
19	O(CH2)5OH	45 ± 17	19 ± 3.7	43		68 ± 61	ND
20	O(CH2CH2O)2H	22 ± 3.7	13 ± 0.77	44		51 ± 21	ND
21		20 ± 1.9	11 ± 0.4	45		37 ± 11	34 ± 20
22		12 ± 0.65	14 ± 0.72	46	4-OC6H4COPh	>111	ND
23		50 ± 15	15 ± 2	47		23 ± 18	17 ± 6.7
24	O(CH2)2PO3Me2	9.0 ± 0.75	17 ± 6.3	48		22 ± 8.5	24 ± 6.6
25	OCH2CH2CN	14 ± 4.5	13 ± 3.7	49		>111	>111
26	OCH2CH2Ph	53 ± 3.1	24 ± 5.5	50	O(CH2)3Br	ND	ND
27	OPh	18 ± 1.1	10 ± 1.6	51	2-OC6H4NHBoc	36 ± 14	ND
28	4-OC6H4OPO3Me2	31 ± 3.5	ND	52	3-OC6H4NHBoc	31 ± 6.4	ND
29	2-OC6H4OH	7.6 ± 2.1	6.6 ± 0.38	53	4-OC6H4NHBoc	88 ± 33	ND
30	3-OC6H4OH	29 ± 20	8.8 ± 1.2	54	O(CH2)2C≡CH	22 ± 3.9	15 ± 0.47
31	2-OC6H4Cl	10 ± 1.6	14 ± 3	55	3-OC6H4C≡CH	43 ± 6.8	13 ± 2.4

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

^b“ND” means “not determined”.