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. 2020 Apr 27;15(14):1310–1321. doi: 10.1002/cmdc.202000136

Table 3.

Phenotypic activity of dihydropyrazolone bio‐isosteres against intracellular amastigotes of T. cruzi (Tulahuen strain) and MRC‐5 cells.

graphic file with name CMDC-15-1310-g019.jpg

Cmpd

Headgroup

pIC50 [a]

SI[b]

T. cruzi

MRC‐5

95

graphic file with name CMDC-15-1310-g020.jpg

4.5

4.3

2

98

graphic file with name CMDC-15-1310-g021.jpg

<4.2

<4.2

99

graphic file with name CMDC-15-1310-g022.jpg

6.3

4.8

32

104

graphic file with name CMDC-15-1310-g023.jpg

5.0

4.6

3

109

graphic file with name CMDC-15-1310-g024.jpg

4.8

<4.2

>4

[a] All reported values are within a standard deviation of ±0.2 and the result of at least n=2. [b] The selectivity index is calculated by dividing the cytotoxicity (IC50) by the T. cruzi activity (IC50).