Table 1.
Antifungal effect of chalcone-based analogues 1–40 against C. albicans control strain.
| Compound | Structure | Inhibition (%) [at 100 μM] | IC50 [μM] a,b | IC50 [μg/mL] a,b |
|---|---|---|---|---|
| 1 |
|
65.2 ± 3.9 | 52.8 [44.6–62.6] | 13.7 [11.5–16.2] |
| 2 |
|
35.8 ± 1.1 | n.d. | n.d. |
| 3 |
|
64.8 ± 1.5 | 57.7 [47.1–70.8] | 16.0 [13.0–19.6] |
| 4 |
|
65.6 ± 3.3 | 48.9 [41.9–57.0] | 13.5 [11.6–15.8] |
| 5 |
|
62.0 ± 1.5 | 51.3 [41.3–63.8] | 15.1 [12.2–18.8] |
| 6 |
|
<1 | n.d. | n.d. |
| 7 |
|
69.0 ± 12.4 | 53.0 [43.8–64.0] | 13.8 [11.4–16.7] |
| 8 |
|
<1 | n.d. | n.d. |
| 9 |
|
38.5 ± 2.9 | n.d. | n.d. |
| 10 c |
|
23.3 ± 9.6 | n.d. | n.d. |
| 11 |
|
9.8 ± 6.7 | n.d. | n.d. |
| 12 c |
|
>99 | 30.7 [27.0–35.0] | 9.0 [7.9–10.3]. |
| 13 c |
|
>99 | 8.1 [6.8–9.6] | 2.4 [2.0–2.8] |
| 14 c |
|
63.6 ± 6.8 | 39.2 [26.8–57.4] | 11.5 [7.9–16.8] |
| 15 |
|
<1 | n.d. | n.d. |
| 16 c |
|
91.9 ± 8.2 | 10.8 [9.3–12.5] | 3.2 [2.7–3.7] |
| 17 |
|
11.0 ± 3.9 | n.d. | n.d. |
| 18 c |
|
34.1 ± 7.5 | n.d. | n.d. |
| 19 |
|
5.9 ± 5.7 | n.d. | n.d. |
| 20 c |
|
81.5 ± 4.7 | 16.8 [13.6–20.6] | 4.9 [4.0–6.0] |
| 21 c |
|
96.5 ± 1.4 | 12.6 [10.6–15.1] | 3.7 [3.1–4.4] |
| 22 c |
|
<1 | n.d. | n.d. |
| 23 |
|
4.6 ± 13.8 | n.d. | n.d. |
| 24 c |
|
72.0 ± 9.8 | 43.8 [30.6–62.7] | 12.8 [9.0–18.4] |
| 25 c |
|
81.3 ± 17.0 | 26.3 [19.6–35.4] | 7.7 [5.7–10.4] |
| 26 c |
|
63.9 ± 3.4 | 36.8 [29.2–46.3] | 10.8 [8.6–13.6] |
| 27 |
|
<1 | n.d. | n.d. |
| 28 |
|
99.1 ± 0.7 | 55.9 [50.9–61.3] | 27.7 [25.2–30.4] |
| 29 |
|
17.8 ± 4.1 | n.d. | n.d. |
| 30 |
|
9.5 ± 4.8 | n.d. | n.d. |
| 31 |
|
97.3 ± 0.5 | 12.0 [9.3–15.6] | 3.5 [2.7–4.6] |
| 32 |
|
<1 | n.d. | n.d. |
| 33 |
|
<1 | n.d. | n.d. |
| 34 |
|
37.9 ± 5.2 | n.d. | n.d. |
| 35 |
|
13.9 ± 3.6 | n.d. | n.d. |
| 36 |
|
<1 | n.d. | n.d. |
| 37 |
|
<1 | n.d. | n.d. |
| 38 |
|
46.3 ± 3.7 | n.d. | n.d. |
| 39 |
|
<1 | n.d. | n.d. |
| 40 |
|
<1 | n.d. | n.d. |
| Licochalcone d | 62.5–150 | 18.3–44.0 | ||
| FLC | n.d. | 0.25 [0.18–0.33] | 0.07 [0.05–0.1] |