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. Author manuscript; available in PMC: 2014 Nov 1.
Published in final edited form as: Bioorg Med Chem. 2013 Aug 20;21(21):10.1016/j.bmc.2013.08.022. doi: 10.1016/j.bmc.2013.08.022

Table 1. In vitro screening data against three different trypanosomatids.

ID No T.b.rhod.a SI T. cruzib SI L.don. axen.c SI Cytotox. L6 Bnz/Comp. Chemical Structure
IC-50 μM IC-50 μM IC-50 μM IC-50 μM
1 1.38 >14 0.34 >562 58.15 >3 >191.1 4.6 graphic file with name nihms519397t1.jpg
2 1.2 99 0.412 287 44.45 3 118.4 3.8 graphic file with name nihms519397t2.jpg
3 5.33 10 0.04 1320 25.92 2 52.79 39.2 graphic file with name nihms519397t3.jpg
4 49.6 5.2 1.678 152 >100 1 >100 0.9 graphic file with name nihms519397t4.jpg
5 35.65 4.3 0.848 180 >315 <1 152.68 1.9 graphic file with name nihms519397t5.jpg
6 1.34 114.6 8.8 17.5 >315 <1 153.9 0.2 graphic file with name nihms519397t6.jpg
7 0.231 180.2 0.048 868 11.35 3.7 41.7 32.7 graphic file with name nihms519397t7.jpg
8 23.85 5.1 0.419 289 173.45 <1 121.34 3.7 graphic file with name nihms519397t8.jpg
9 35.56 3.5 0.556 224.5 >238.66 <1 124.8 2.8 graphic file with name nihms519397t9.jpg
10 10.46 10.8 0.828 137 180.2 <1 113.3 2.5 graphic file with name nihms519397t10.jpg
11 0.78 42.9 0.286 117 23.9 1.4 33.5 7.1 graphic file with name nihms519397t11.jpg
12 15.62 13 4.7 43.1 >290 <1 202.9 0.3 graphic file with name nihms519397t12.jpg
13 62.4 2.2 34.4 4 186.4 <1 137.1 0.1 graphic file with name nihms519397t13.jpg
14 10.74 7.4 9.4 8.4 149.5 <1 79.2 0.2 graphic file with name nihms519397t14.jpg
15 0.204 500 0.059 1725 4.49 22.7 101.9 26.6 graphic file with name nihms519397t15.jpg
16 0.954 170 0.566 287 20 8.1 162.5 3.6 graphic file with name nihms519397t16.jpg
17 0.355 125.6 0.142 314 4.1 10.9 44.54 14.4 graphic file with name nihms519397t17.jpg
18 7.61 6.5 3.23 15.3 4.27 11.6 49.5 0.6 graphic file with name nihms519397t18.jpg
19 52.5 3.4 4.88 36.1 11.4 15.4 176 0.4 graphic file with name nihms519397t19.jpg
20 3.87 11.1 1.75 24.6 7.3 5.5 43 1.2 graphic file with name nihms519397t20.jpg
a

STIB 900 trypomastigotes;

b

Tulahuen C4 amastigotes;

c

MHOM-ET-67/L82 amastigotes; Cytotoxicity was measured in L6 cells. SI = IC50 in L6 cells / IC50 in each type of parasites. The reference compounds were: Melarsoprol (T. b. rhodesiense; IC50 = 0.011 0.004), Benznidazole (Bnz; T. cruzi; IC50 = 1.85 0.33) and Miltefosine (L. donovani; IC50 = 0.378 0.011). Bnz/comp.: The ratio of IC50 values of Benznidazole and each tested compound against T. cruzi. The IC50 values are the means of two independent assays and varies less than ± 50%. Green color indicates active compounds, light red, moderately active, light blue, toxic and no color, inactive. Compounds 1-3 have been described before [10].