Table 2.
Phenotypic activity of analogues with gem‐dimethyl modifications against intracellular amastigotes of T. cruzi (Tulahuen strain) and MRC‐5 cells.
|
| ||||
|---|---|---|---|---|
|
Cmpd |
R |
pIC50 [a] |
SI[b] |
|
|
|
|
T. cruzi |
MRC‐5 |
|
|
89 |
|
5.2 |
4.5 |
5 |
|
90 |
|
5.1 |
4.4 |
5 |
|
91 |
|
4.5 |
4.3 |
2 |
|
92 |
|
4.5 |
4.5 |
1 |
[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).