Table 1.
Bioactivity and cytotoxicity profiles of organotin (IV) derivatives against different parasites and mammalian cell lines. For S. mansoni, the data display the least concentration at which a severity score of 4 was recorded after 24 h. Background color: a range of color from green to red was set for each cell or parasite. Green refers to low cytotoxicity to host cells or potent antiparasitic activity; red refers to high cytotoxicity to host cells or weak/non-observed antiparasitic activity up to the highest tested concentration.
| Compounds | MW | CC50 (µM) | EC50 (µM) | SI Index | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| C2C12 | HEK923 | B10R | L. donovani (pro) | L. donovani ntracelular amastigotes | T. cruzi (infecting C2C12) | T. brucei | E. histolytica | G. lamblia | N. fowleri | S. mansoni, adult worm | SIa | SIb | SIC | ||
| MS26 | 223.23 | >20.0 | >4.00 | 2.38 | >20.0 | 1.08 | 3.21 | >4.0 | >10.0 | >10.0 | >10.0 | >10.0 | 2.02 | 6.23 | 1 |
| MS26Na | 245.1 | 1.61 | >4.00 | 4.55 | 0.17 | 3.88 | 4.27 | >4.0 | >10.0 | >10.0 | >10.0 | >10.0 | 1.06 | 0.38 | 1 |
| MS26Me3 | 386.03 | 9.41 | 1.24 | 4.87 | >20.0 | 3.26 | >20.0 | >4.0 | >10.0 | >10.0 | >10.0 | 10 | 1.45 | 0.47 | 0.31 |
| MS26Et3 | 428.11 | 2.79 | 0.56 | 2.41 | 0.21 | 0.19 | 0.24 | 0.09 | 5.6 | 8 | 1.4 | 5 | 13.1 | 11.7 | 6.22 |
| MS26Bu3 | 512.3 | 0.22 | 0.14 | 0.17 | 0.22 | 0.21 | 0.11 | 0.05 | 8.7 | 1.03 | 1.5 | 1.25 | 0.8 | 2 | 2.8 |
| MS26Ph3 | 572.24 | 0.41 | 0.36 | 0.29 | 0.39 | 9.1 | >20.0 | 0.09 | >10.0 | 5.3 | 3.2 | 1.25 | 0.1 | 0.03 | 4 |
| MS26Cy3 | 590.38 | >20.0 | 0.11 | 0.11 | >20.0 | >20.0 | 0.3 | 0.08 | >10.0 | >10.0 | 7.5 | 1.25 | 0.01 | 66 | 1.37 |
| MS26Bu2 | 677.4 | 0.14 | 0.37 | 1.06 | 0.76 | 0.28 | 0.53 | 0.29 | >10.0 | >10.0 | >10.0 | 1.25 | 3.78 | 0.27 | 1.28 |
| MS26Oct2 | 789.59 | >20.0 | >4.00 | >20.0 | >20.0 | >20.0 | >20.0 | >4.0 | >10.0 | >10.0 | >10.0 | >10.0 | 1 | 1 | 1 |
| MS26vin2 | 617.2 | >20.0 | >4.00 | >20.0 | >20.0 | >20.0 | >20.0 | >4.0 | >10.0 | >10.0 | >10.0 | >10.0 | 1 | 1 | 1 |
| MS26(1,10-Ph) | 566.24 | >20.0 | >4.00 | 6.25 | >20.0 | >20.0 | 13.6 | >4.0 | >10.0 | >10.0 | >10.0 | >10.0 | 1 | 1.48 | 1 |
| MS26BuSnCl2 | 468.95 | 18.1 | >4.00 | 0.62 | >20.0 | >20.0 | >20.0 | >4.0 | >10.0 | >10.0 | >10.0 | >10.0 | 0.031 | 0.91 | 1 |
| AmpB | 0.09 | ||||||||||||||
| Benznidazole | 4.71 | ||||||||||||||
| Pentamidine | 0.01 | ||||||||||||||
| Metronidazole | 4.4 | 5.7 | |||||||||||||
| Praziquantel | 1.25 | ||||||||||||||
SIa: Calculated ratio between CC50 in B10 R cells and EC50 against L. donovani intracellular amastigotes. SIb: The ratio between CC50 in C2C12 cell lines and EC50 against T. cruzi intracellular amastigotes. SIc: The ratio calculated between CC50 in HEK923 cell lines and EC50 against T. brucei.