TABLE 2.
The antiproliferative activities, cytotoxicity, selectivity index and resistance index values of 1,2,3-triazole tethered dihydroartemisinin-isatin hybrids 8a-c and 9a-k.
| Compd | IC50 (μM) | SI a | RI | ||||
|---|---|---|---|---|---|---|---|
| A549 | A549/DOX b | A549/DDP c | NIH/3T3 | RI1 d | RI2 e | ||
| 8a | 8.32 | 12.1 | 10.7 | >100 | >12.0 | 1.45 | 1.29 |
| 8b | 21.6 | 32.0 | 19.5 | >100 | >4.6 | 1.48 | 0.90 |
| 8c | 7.54 | 9.89 | 8.77 | >100 | >13.2 | 1.31 | 1.16 |
| 9a | 16.3 | 38.4 | 30.9 | >100 | >6.1 | 2.35 | 1.90 |
| 9b | 12.0 | 26.1 | 30.3 | >100 | >8.3 | 2.18 | 2.52 |
| 9c | 22.7 | 19.5 | 27.4 | >100 | >4.4 | 0.86 | 1.20 |
| 9d | 25.6 | 20.8 | 33.7 | >100 | >3.9 | 0.81 | 1.32 |
| 9e | 16.3 | 31.4 | 29.9 | >100 | >6.1 | 1.92 | 1.83 |
| 9f | 65.4 | 79.5 | 51.8 | >100 | >1.5 | 1.22 | 0.79 |
| 9g | 73.8 | 45.0 | 61.7 | >100 | >1.3 | 0.61 | 0.84 |
| 9h | 44.7 | 77.7 | 59.4 | >100 | >2.2 | 1.74 | 1.33 |
| 9i | 9.10 | 15.9 | 14.3 | >100 | >11.0 | 1.75 | 1.57 |
| 9j | 9.61 | 13.0 | 38.2 | >100 | >10.4 | 1.35 | 3.98 |
| 9k | 15.8 | 31.1 | 28.7 | >100 | >6.3 | 1.97 | 1.82 |
| Artemisinin | >100 | >100 | >100 | >100 | - | - | - |
| DHA f | 69.4 | 88.0 | 75.9 | >100 | >1.4 | 1.27 | 1.09 |
| cisplatin | 9.38 | 19.7 | 66.9 | >100 | >10.6 | 2.10 | 7.13 |
b
Doxorubicin-resistant A549 cells.
c
Cisplatin-resistant A549 cells.
a
Selectivity index: IC50(NIH/3T3)/IC50(A549).
d
Resistance index: IC50(A549/DOX)/IC50(A549).
e
Resistance index: IC50(A549/DDP)/IC50(A549).
f
Dihydroartemisinin.