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. 2020 Oct 13;6(11):2872–2878. doi: 10.1021/acsinfecdis.0c00523

Table 2. Anti-T. cruzi Activity and Mammalian Cytotoxicity of Synthetic Analogues with a Variation of S1 Substitutiona.

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      IC50 (μM) ± SDb
   
entry compound S1 trypomastigote amastigote CC50 (μM) ± SDc SId
1 1e OH 38.6 ± 8.3 86.5 ± 16.2 >200 >2.3
2 2e OMe NA NA >200 ND
3 5 OMOM 6.5 ± 4.9 24.4 ± 10.3 >200 >8.2
4 6 OPMB NA 4.0 ± 1.4 >200 >50
5 7f OAllyl NA NA >200 ND
6 8f OBn NA 9.5 ± 1.3 >200 >21.1
7 25 H NA 10.9 ± 6.5 >200 >18.3
8 benznidazole   17.7 ± 1.9 5.0 ± 1.5 190.6 ± 13.4 38.1
a

SD: standard deviation; ND: not determined; NA: not active.

b

IC50: 50% inhibitory concentration.

c

CC50: 50% cytotoxic concentration.

d

SI: selectivity index, given by the ratio between CC50 in NCTC cells and IC50 in intracellular amastigotes.

e

Published in ref (18).

f

Published in ref (20).