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. 2017 Jul 31;8(10):1872–1890. doi: 10.1039/c7md00280g

Table 1. In vitro and in vivo data from compounds mentioned herein.

Compd T. brucei IC50 [μM| Cytotoxicity CC50 [μM] SI in vivo infection Treatment regime Curation Lit.
6 0.89 a >213 c >240 T. b. rhodesiense STIB900 20 mg kg–1, ip, for 4 days, begin 3 days pi 4/4 28
T. b. brucei GVR35 50 mg kg–1, ip, for 5 days, begin 17 days pi 1/5
7 0.009 a 69 c 7667 T. b. brucei Lab 110 EATRO 10 mg kg–1, ip, for 3 days, begin 1 day pi 3/3 40
0.096 b
T. b. rhodesiense Ketri 2538 3/3
8 0.003 a 100 c 33 333 T. b. brucei Lab 110 EATRO 5 mg kg–1, ip, for 3 days, begin 1 day pi 3/3 40
0.002 b
T. b. rhodesiense Ketri 2538 3/3
9 0.002 a 43 c 21 500 T. b. brucei Lab 110 EATRO 1 mg kg–1, ip, for 3 days, begin 1 day pi 3/3 40
0.002 b
T. b. rhodesiense Ketri 2002 3/3
10 0.0077 a >100 d >13 000 T. b. brucei Lister 427 3 mg kg–1, ip, qd, for 4 days, 5/5 41
>100 e
11 0.002 a 0.3 f 150 T. b. brucei S427 12.5 mg kg–1, po, bid, for 4 days, begin 3 days pi 5/5 46
T. b. rhodesiense STIB900 50 mg kg–1, po, bid, for 2 days, begin 3 pi 5/5
T. b. brucei GVR35 100 mg kg–1, po, bid, for 5 days, begin 21 pi 0/5 45
12 0.001 a 1 f 1000 T. b. brucei S427 50 mg kg–1, po, bid, for 4 days, begin 3 days pi 5/5 47
T. b. brucei GVR35 100 mg kg–1, po, bid, for 5 days 0/5
50 mg kg–1, po, bid, for 10 days 0/5
100 mg kg–1, po, bid, for 8 days 1/5
100 mg kg–1, po, bid, for 3 rounds of 3 day treatment with a two day hiatus between rounds 1/5
14 0.002 a 30 e >15 000 T. b. rhodesiense STIB9000 5 mg kg–1, po, bid, for 5 days, begin 2 days pi 5/5 52
24 g
15 0.07 a >20 h >286 T. b. brucei GVR35-VSL2 100 mg kg–1, qd, oral gavage, for 7 days, begin 21 days pi 6/6 53
>50 i >714
16 0.191 a 103 c 539 T. b. rhodesiense STIB900 50 mg kg–1, ip, bid, for 3 days, begin 1 day pi 0 54
0.632 b 162
17 0.0348 a >50 g >1437 T. b. rhodesiense STIB900 50 mg kg–1, po, bid, for 4 days, begin 2 days pi 5/5 55
>50 e
>1437
T. b. brucei TREU667 50 mg kg–1, po, bid, for 10 days, begin 21 days pi 5/5 55
18 0.03 a >50f >1800 T. b. brucei S427 10 mg kg–1, ip, bid, for 4 days 2/3 56
19 0.06 a >50 f >860 T. b. brucei GVR35 12.5 mg kg–1, ip, bid, for 5 days, begin 21 days pi 1/5
20 0.120 a 25 j 213 T. b. brucei 20 mg kg–1, ip, qd, for 5 days, begin 1 day pi 2/4 57
25 k
25 mg kg–1, ip, bid, for 10 days, begin 1 day pi 4/4
21 0.590 a 16.8 Data not shown; according to ref. 21 0/4 59
0.200 b
0.01 (Tbg)
22 0.0059 a T. b. rhodesiense STIB900 200 mg kg–1, ip, qd, for 4 days, begin 3 days pi 0/4 61
23 0.0163 a T. b. rhodesiense EATRO3 10 mg kg–1, ip, qd, for 4 days begin 3 days pi 0/5 62
0.00073 b
24 0.00096 a 12 f 12 500 T. b. rhodesiense TREU164 10 mg kg–1, ip, bid, for 4 days – 4 days hiatus – 4 days; begin 3 days pi 4/4 66
T. b. brucei Lister 427 3/4
T. b. brucei GVR35 20 mg kg–1, ip, bid, for 4 days – 4 days hiatus – 4 days; begin 3 day pi 0/5 67
25 1.5 a >20 l >13 T. b. brucei CA427 100 mg kg–1, po, bid, for 14 days, begin 1 day pi 1/4 71
26 1 a 301 d 293 T. b. brucei s427 3 mg kg–1, ip, qd, for 4 days 11 days max survival 75
27 1 a 65 d 62 8 days max. survival
30 6.03 (Tbg) >30 m 5 T. b. brucei CMP 100 μmol kg–1, ip, qd, 0/6 77
31 0.047 a 47.2 c 1004 T. b. rhodesiense STIB900 3.5 mg kg–1, ip, bid, for 4 days, begin 3 days pi Mean survival 17 days 79
0.001 b 57.0 i 1212
26.3 d 560
47.0 e 1001 3.5 mg kg–1, ip, bid, for 4 days, begin 1 day pi, 3/6
32 0.0023 a 9.19e 3916 T. b. brucei Lister 427 20 mg kg–1, iv, for 6 days, begin 3 days pi 0/4 84
30 mg kg–1, ip, qd, begin 1 day pi,
33 0.82 a 192 d 234 T. b. brucei Lister 427 400 mg kg–1, po, qd, 4 days, begin 1 day pi 0/4 87
34 0.68 a 92.4 d 136 200 mg kg–1, oral gavage, qd, 4 days, begin 1 day pi 0/4 87
35 0.0031 a 1 n 300 T. b. brucei MiTat1.2 s427 30 mg kg–1, ip, qd, begin 1 day pi, 3/3 88
50 mg kg–1, po, qd, begin 1 day pi 2/3
36 0.022 b 0.146 c 6 T. b. rhodesiense STIB900 50 mg kg–1, ip, qd, 4 days Relapse on day 11 90
37 0.0018 b 0.201 c 11 Relapse on day 9 90
39 0.45 a 15.7 d 35 T. b. brucei TC221 5 mg kg–1, ip, qd, for 30 days, begin 5 days pi 92
40 0.038 a 12.9 d 340 T. b. brucei S427 50 mg kg–1, ip, qd, for 4 days, begin 2 days pi 0/3 93
41 0.055 a 2.1 e 38 T. b. brucei RUMP528 40 mg kg–1, po, qd, total 14 doses (4 days on/2 days off), begin 1 day pi 4/4 94
0.058 b
42 0.430 a 4.7 o 11 T. b. brucei TC-221 30 mg kg–1, ip, qd, for 5 days, begin 6 h pi 5/5 97
10.9 p 25

a T. b. brucei.

b T. b. rhodesiense.

cL6 rat myoblasts.

dHEK293T human embryonic kidney cells.

eHepG2 human hepatocytes.

fMRC5 human lung fibroblasts.

gCRL-8155 human lymphoblasts.

h3T3 fibroblasts.

iMacrophages.

jMOLT4 human T lymphoblasts.

kL929 fibroblasts.

lHeLa cells.

m3T6 fibroblasts.

nL1210 lymphocytic B-cells.

oSkin fibroblasts.

pLung fibroblasts.