Table 2.
Summary of modifications to the aldehyde.
| # | R1 | R3 | R4 | TAO inhibition (pIC50)a | T.b.b. Growth inhibition (pIC50)b | HepG2 Cytotox (pCC50)c |
|---|---|---|---|---|---|---|
| 29 | OH | Me | CN | 8.4 ± 0.2 | 6.4 ± 0.1 | 4.9 ± 0.1 |
| 6 | OH | Me | C=O | 8.5 ± 0.3 | 8.4 ± 0.1 | 5.1 ± 0.1 |
| 20 | OAc | Me | C=O | 6.5 ± 0.2 | 7.4 ± 0.7 | 4.8 ± 0.1 |
| 30 | OAc | Me | Me | 5.7 ± 0.1 | – | – |
| 21 | OH | H | C=O | 7.0 ± 0.2 | 6.6 ± 0.1 | <4.8 |
| 31 | OH | H | CN | 7.6 ± 0.3 | 5.2 ± 0.1 | 4.4 ± 0.1 |
| 32 | OH | H | C=NOH | 6.1 ± 0.3 | 5.7 ± 0.1 | 5.0 ± 0.1 |
a
Negative log concentration and standard deviation of compounds required for 50% inhibition of trypanosome alternative oxidase.
b
Negative log concentration and standard deviation of compounds required for 50% growth inhibition of T. b. brucei Lister427.
c
Negative log concentration and standard deviation of compounds required for 50% growth inhibition of HepG2 cell line.