Table 2.
Chalcone derivatives investigated against HIV.
| Compound(s) “Chemical name(s)” | Virus subtype | Study model(s) | Results | Inhibition mechanism | Refs. |
|---|---|---|---|---|---|
| Glabarachalcone “(E)-1-7(7-hydroxhy-2-2dimethyl chromen-6-yl)-3-phenylprop-2-en-1-one” | HIV-1 | In silico, In vitro | Mean inhibition against HIV gag p24: 66.9 ± 4.4% | Potent binding to RT enzyme and P24 protein , inhibition of HIV-1 gag p24 |
[68] |
| Quinoline-based chalcones | HIV-1 | In silico, In vitro | IC50 (the most active compounds): 0.10 and 0.11 μg/mL; binding free energies (ΔG): 9.30 and −9.13 kcal |
Inhibition of RT (non-nucleoside reverse transcriptase) | [69] |
| A series of ferrocenyl chalcone borates | HIV-1 | In vitro | IC50: 4–16 μM (for 3′ processing activities) and 0.7–9 μM (for strand transfer activities) | Inhibition of the IN 3′ processing and strand transfer steps | [73] |
| Amt-87 “(E)-3-(5-(adamantan-1-yl)-2,4-bis (methoxymethoxy) phenyl)-1-(2-hydroxy-5-methylphenyl)prop-2-en-1-one” | HIV-1 | In vitro | Stimulated GFP expression in J-Lat A2 cells at concentrations of 50 and 100 μg/mL | Latency-reversing agent (LRA) | [75] |
| Hydroxypanduratin A “(1R,2S,6R)-3-methyl-2-(3-methylbut-2-enyl)-6-phenylcyclohex-3-en-1-yl]-(2,4,6-trihydroxyphenyl)methanone” panduratin A “(2,6-dihydroxy-4-methoxyphenyl)-[(1R,2S,6R)-3-methyl-2-(3-methylbut-2-enyl)-6-phenylcyclohex-3-en-1-yl]methanone” | HIV-1 | In vitro | IC50: 5.6 and 18.7 μM, respectively | Suppression of HIV-1 protease | [79] |
| Cardamonin “(E)-1-(2,4-dihydroxy-6-methoxyphenyl)-3-phenylprop-2-en-1-one” | HIV-1 | In vitro | IC50 of 31 μg/mL | Inhibition of HIV-1 protease | [80] |
HIV: Human immunodeficiency virus, IC50: Half maximal inhibitory concentration.