Table 1.
Leishmanicidal and cytotoxic activities of sulfonamides that showed antileishmanial activity in any of the parasite stages.
| Compound |
Leishmania infantum |
U937 10 μM |
HT-29 1 μM |
HeLa 1 μM |
MC7 1 μM |
||
|---|---|---|---|---|---|---|---|
| Promastigotes |
Axenic amastigotes |
Intracellular amastigotes |
|||||
| 10 μM | IC50 (μM) | 20 μM | |||||
| 129 | NA | 0.93 | A | NC | NC | NC | NC |
| 138 | NA | NA | A | NC | NC | NC | NC |
| 204 | NA | 2.2 | ND | C | C | C | C |
| 183 | NA | NA | A | NC | NC | NC | NC |
| 332 | NA | 4.3 | ND | C | C | C | C |
| 326B | NA | 8.2 | ND | C | C | C | C |
| 275 | NA | 8.1 | ND | C | NC | NC | NC |
| 242 | NA | NA | A | NC | NC | NC | NC |
| 320 | NA | NA | A | NC | NC | NC | NC |
| 316 | NA | NA | A | NC | NC | NC | NC |
| 279 | NA | 12 | NA | NC | NC | NC | NC |
| 334 | NA | 5.75 | NA | NC | NC | NC | NC |
| 124 | NA | NA | A | NC | NC | NC | NC |
| 132 | NA | NA | A | NC | NC | NC | NC |
| 117 | NA | NA | A | NC | NC | NC | NC |
| 35 | NA | NA | A | NC | NC | NC | NC |
| 26 | NA | NA | A | NC | NC | NC | NC |
| 84 | NA | NA | A | NC | NC | NC | NC |
| 90 | NA | NA | A | NC | NC | NC | NC |
| 147 | NA | NA | A | NC | NC | NC | NC |
| 63B | NA | NA | A | NC | NC | NC | NC |
| 276B | NA | 6.7 | A | NC | NC | NC | NC |
| Miltefosine | A | 4.4 | A | NC | ND | ND | ND |
Leishmanicidal activities of sulfonamides on L. infantum promastigotes and axenic amastigotes at 10 μM and IC50 calculation; on intracellular amastigotes at 20 μM and cytotoxicity on human tumor cell lines U937 at 10 μM and HT-29, HeLa and MCF7 at 1 μM. NA, Inactive at tested concentration. A, Active at tested concentration. NC, Not Cytotoxic at tested concentration. C, Cytotoxic at tested concentration. ND, Undetermined. Assays are described in Materials and Methods.