Table 2.

In vitro drug sensitivity against drug-resistant T. brucei.

Cpd.	Lister 427 EC50 (µM)	TbAT1-KO EC50 (µM)	RF	B48 EC50 (µM)	RF	ISMR1 EC50 (µM)	RF
6 TUB	0.15 ± 0.03	2.61 ± 0.70	17.2**	4.3 ± 1.3	28.7*	1.7 ± 0.5	11.1**
8 7-Br-TUB	0.32 ± 0.27	0.825 ± 0.0173	2.62***	0.448 ± 0.196	1.42	1.529 ± 0.157	4.85**
9 3′-Deoxy-TUB	0.033 ± 0.001	0.375 ± 0.012	11.2***	0.368 ± 0.013	11.0***	0.0324 ± 0.0038	0.97
10 7-Br-3′-deoxy-TUB	0.0018 ± 0.0003	0.0021 ± 0.00025	1.2	0.0013 ± 0.0003	0.75	0.0011 ± 0.0002	0.63
11 2′-Deoxy-TUB	96.4 ± 13.8	43.7 ± 2.2	0.45**	41.8 ± 1.4	0.43**	77.8 ± 1.7	0.81
12 7-Br-2′-deoxy-TUB	0.31 ± 0.063	0.76 ± 0.18	2.37*	0.83 ± 0.16	2.64**	0.92 ± 0.12	2.93**
Pentamidine	0.011 ± 0.001	0.018 ± 0.002	1.8**	0.99 ± 0.16	94.6***	0.14 ± 0.04	13.8**
Diminazene	0.42 ± 0.064	4.5 ± 0.9	10.6***	7.2 ± 1.6	16.9***	2.9 ± 0.4	6.9***
Isometamidium	0.65 ± 0.085	0.75 ± 0.14	1.2	0.56 ± 0.13	0.85	3.1 ± 0.5	4.8***

In vitro antitrypanosomal evaluation against drug-resistant T. b. brucei cell lines. EC₅₀ values are given in µM and are mean and SEM of three independent determinations (n = 3). RF = Resistance factor, that is, the ratio of EC₅₀ of resistant and reference (Lister 427WT) cell line. TbAT1-KO: T. brucei cell line lacking the TbAT1(P2) transporter gene. B48: pentamidine, diminazene and melaminophenyl arsenical resistant T. brucei line. ISMR1: isometamidium-resistant T. brucei cell line. TUB, tubercidin. Source data are provided as a Source Data file

*p <0.05, **p <0.01; ***p < 0.001; Student’s t test (two-sided)