Table 5.
Antifungal activity and cytotoxicity of the head-to-tail bisindole analogs with varied core structures
| # | Structure | MIC (μg/ml)† | |||||
|---|---|---|---|---|---|---|---|
|
C. alb | C. kru | C. gla | C. par | C. neo | CC50 (μg/ml) | |
| P32 |
|
0.5 | 0.5 | 0.13 | 0.5 | 2 | 34.6 |
| P33 |
|
0.79 | 1 | 0.13 | 0.31 | 0.5 | 13.4 |
| P34 |
|
0.25 | 0.5 | 0.06 | 0.13 | 0.13 | 1.5 |
| P35 |
|
16 | 16 | 32 | 8 | 1 | 20.7 |
| P36 |
|
8 | 8 | 1.59 | 2.52 | 3.94 | 32.5 |
| P37 |
|
2 | 8 | 0.31 | 2 | 2 | 25.5 |
| P38 |
|
4 | 8 | 1 | 0.79 | 1 | 20.7 |
| P39 |
|
4 | 25.4 | 2.52 | 2 | 1 | 40.5 |
| P40 |
|
3.17 | 16 | 5.04 | 2 | 4 | 27.5 |
| P41 |
|
0.31 | 4 | 0.13 | 0.5 | 0.5 | 17.1 |
| P42 |
|
0.4 | 4 | 1 | 0.5 | 1 | 50.5 |
| P43 |
|
1 | 1.26 | 0.16 | 1 | 6.25 | 91.9 |
MICs are the geometric mean of three independent assays, MIC values < 1 μg/ml are in blue.
Fungal strains: C. alb, Candida albicans (WTBF-50); C. kru, Candida krusei (WTBF-51); C. gla, Candida glabrata (WTBF-86); C. par, Candida parapsilosis (WTBF-88); C. neo, Cryptococcus neoformans Cn18 (WTBF-106).