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. 2020 Oct 1;25(19):4510. doi: 10.3390/molecules25194510

Table 1.

Antileishmanial, antitrypanozomal and cytotoxic activity of the synthesised derivatives, compared to the positive controls Benznidazole and Miltefosine. The IC50 values are given in mM as average data, with the standard deviations from at least three independent experiments. See Experimental for details about the assays.

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Mol. R6′ R6′’ R1 R2 R3 T. cruzi L. brasiliensis L. amazoniensis Cytotoxicity a
IC50 (μM) SI b IC50 (μM) SI b IC50 (μM) SI b IC50 (μM)
1 Me Me H OMe H 18.5 ± 9.6 1.7 59.2 ± 11.8 0.5 77.7 ± 5.5 0.4 30.7 ± 1.1
8a H H H OMe H 66.0 ± 18.2 1.3 248.1 ± 54.1 0.3 132.1 ± 29.3 0.6 82.6 ± 9.5
8b Me H H OMe H 35.9 ± 11.7 1.0 156.1 ± 23.4 0.2 156.1 ± 58.5 0.2 37.1 ± 3.9
8c H Me H OMe H 67.1 ± 31.2 0.8 128.8 ± 24.6 0.4 71.8 ± 12.5 0.7 52.7 ± 9.0
8d Et H H OMe H 51.8 ± 9.2 0.6 45.9 ± 20.3 0.7 71.4 ± 1.1 0.4 30.0 ± 3.7
8e H Et H OMe H 37.0 ± 0.7 1.2 45.1 ± 19.2 1.0 70.3 ± 3.7 0.6 44.4 ± 11.5
8f Et Et H OMe H 10.4 ± 0.3 4.2 46.9 ± 5.0 0.9 36.9 ± 3.4 1.2 43.6 ± 15.1
8g Bu Bu H OMe H 22.8 ± 8.5 1.5 29.3 ± 1.4 1.2 25.4 ± 1.1 1.4 35.3 ± 17.5
10a Me Me H H OMe 88.4 ± 12.2 0.7 37.4 ± 1.1 1.6 66.6 ± 7.4 0.9 59.2 ± 25.9
10b Me Me OMe H H 92.5 ± 14.8 0.5 48.1 ± 18.5 1.0 179.8 ± 21.9 0.3 48.1 ± 18.5
10c Me Me H Me H 31.5 ± 7.9 1.3 39.3 ± 2.4 1.0 64.9 ± 12.6 0.6 39.3 ± 1.6
10d Me Me H H Me 33.0 ± 3.9 1.1 40.1 ± 8.3 0.9 51.9 ± 13.8 0.7 35.4 ± 7.9
10e Me Me H H H 50.8 ± 6.2 1.2 74.9 ± 16.6 0.8 91.6 ± 5.4 0.7 62.4 ± 6.2
10f Me Me H i-Pr H 12.4 ± 3.5 0.7 18.1 ± 0.7 0.5 15.6 ± 2.8 0.6 8.9 ± 3.5
10g Me Me H H i-Pr 14.2 ± 4.2 1.6 19.1 ± 1.1 1.1 21.2 ± 7.1 1.0 22.0 ± 7.1
10h Me Me H n-Pen H 6.4 ± 0.3 2.0 16.4 ± 0.3 0.8 16.8 ± 1.9 0.8 12.9 ± 3.2
Benznidazole 19.2 ± 7.7 3.9 - - - - 74.7 ± 9.1
Miltefosine - - 13.0 ± 1.2 5.9 10.8 ± 1.5 7.1 76.6 ± 3.2

a Toxicity was measured on RAW cells, see Experimental for details, b SI, selectivity index (cytotoxicity/anti-protozoal activity).