2. Cytotoxic Activity of BQACs (Series 5–7) against Pancreatic Cancer and Normal Cell Lines.
| IC50 (μM)
|
||||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Series | Compound | KP4 | PANC1 | IMR90 | hTerT-HPNE | S.I. IMR90/KP4 | S.I. HPNE/KP4 | S.I. IMR90/PANC1 | S.I. HPNE/PANC1 | Clog P |
| Series 5 | 17 | 9 ± 1 | ND | 26 ± 7 | ND | 2.9 | ND | ND | ND | 1.0 |
| 18 | 4.5 ± 0.4 | ND | 16 ± 5 | ND | 3.6 | ND | ND | ND | 1.3 | |
| 19 | 1.16 ± 0.07 | ND | 7 ± 1 | ND | 6.0 | ND | ND | ND | 1.7 | |
| 20 | 2.3 ± 0.2 | ND | 6 ± 2 | ND | 2.6 | ND | ND | ND | 1.5 | |
| 21 | 1.1 ± 0.3 | ND | 2.90 ± 0.01 | ND | 2.6 | ND | ND | ND | 2.7 | |
| Series 6 | 22 | >285 | ND | >285 | ND | ND | ND | ND | ND | 0.99 |
| 23 | 24 ± 4 | 145 ± 10 | >285 | >285 | >12 | >12 | >2.0 | >2.0 | 1.6 | |
| 24 | 11 ± 1 | ND | 99 ± 19 | ND | 9.0 | ND | ND | ND | 2.4 | |
| 25 | 202 ± 54 | ND | >285 | ND | 1.4 | ND | ND | ND | 2.0 | |
| 26 | 6.6 ± 0.9 | 121 ± 13 | >285 | >285 | >43 | >43 | >2.4 | >2.4 | 3.2 | |
| Series 7 | 27 | 78 ± 5 | ND | 244 ± 26 | ND | 3.1 | ND | ND | ND | –0.03 |
| 28 | 56 ± 9 | ND | 276 ± 52 | ND | 4.9 | ND | ND | ND | 0.79 | |
| 29 | 19 ± 3 | ND | 156 ± 49 | ND | 8.2 | ND | ND | ND | 1.3 | |
| 30 | 100 ± 9 | ND | 829 ± 190 | ND | 8.3 | ND | ND | ND | 1.2 | |
| 31 | 1.8 ± 0.2 | 17 ± 2 | 172 ± 11 | >285 | 96 | >158 | 10 | >17 | 2.3 | |
a
IC50 values are the mean of three independent triplicates.
b
S.I. Selectivity index = IC50 value of normal cell line over IC50 value of cancer cell line.
c
Consensus on the calculated log P from Swiss ADME.
d
ND: not determined.