Research Article
Copper- and Ligand-Free Sonogashira Cross-Coupling: Access to Novel 3-Aminoindole Derivatives and Their Biological Evaluations
Table 3
Anti-Mycobacterium tuberculosis, antiplasmodial, and cytotoxicity assays of the 3-aminoindole derivatives 10a–t.
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| | Structure | MIC90 (μM) Mtb H37RV strain | % Survival
Plasmodium falciparum (Nf54) | Cytotoxicity
IC50 (μg/ml) | | 7H9_CAS_GLU TX | 7H9_ADC_GLU TX | Raw 264.7 mouse macrophages | Skin KMST-6 human cells | Kidney Hek-293 human cells |
| | 10a | 7.813 | >125 | 77.5 | >100 | >100 | >100 | | 10b | 125 | >125 | 80.7 | >100 | >100 | >100 | | 10c | — | 21.590 | 70.3 | >100 | >100 | >100 | | 10d | 15.625 | >125 | 88.9 | >100 | >100 | >100 | | 10e | 7.955 | 15.503 | 84.9 | >100 | >100 | >100 | | 10f | 21.874 | >125 | 84.1 | >100 | >100 | >100 | | 10g | 125 | >125 | 85.6 | >100 | >100 | >100 | | 10h | — | 62.5 | 83.1 | >100 | >100 | >100 | | 10i | 125 | 17.076 | 85.9 | >100 | >100 | >100 | | 10j | >125 | 8.332 | 65.6 | >100 | >100 | >100 | | 10k | >125 | >125 | 76.5 | >100 | >100 | >100 | | 10l | 125 | >125 | 76.3 | >100 | >100 | >100 | | 10m | 125 | >125 | 81.3 | >100 | >100 | >100 | | 10n | 62.5 | >125 | 82.6 | >100 | >100 | >100 | | 10o | 62.5 | 15.373 | 85.1 | >100 | >100 | >100 | | 10p | >125 | >125 | 77.8 | >100 | >100 | >100 | | 10q | 32.354 | 62.5 | 87.1 | >100 | >100 | >100 | | 10r | 31.864 | 125 | 78.8 | >100 | >100 | >100 | | 10s | 9.514 | 16.043 | 77.5 | >100 | >100 | >100 | | 10t | — | 20.970 | 81.1 | >100 | >100 | >100 | | Rifampicin | 0.001 | 0.02 | — | | | | | Chloroquine | — | — | 0.007 | | | | | Curcumin (μM) | — | — | — | 50 | 50 | 52.5 |
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