Table 3.
GI50 values (μM) of compounds 7 and 19 compared with those of erlotinib, gefitinib, and 5-FU on in vitro subpanel tumour cell lines.
| Subpanel tumour cell lines | GI50 (μM) | ||||
|---|---|---|---|---|---|
| 7 | 19 | Erlotinib | Gefitinib | 5-FU | |
| Leukaemia | |||||
| CCRF-CEM | 4.91 | >100 | 15.84 | 5.01 | 31.62 |
| HL-60(TB( | 3.57 | >100 | 5.01 | 5.01 | 19.95 |
| MOLT-4 | 7.38 | >100 | 5.01 | 3.98 | 12.58 |
| RPMI-8226 | 4.00 | 22.90 | 5.01 | 1.58 | 5.01 |
| SR | 3.01 | 18.05 | 6.30 | 3.16 | 3.98 |
| Non-small cell lung cancer | |||||
| A549/ATCC | 6.33 | 4.66 | 7.94 | 7.94 | 1.99 |
| HOP-62 | 4.36 | 3.10 | 12.58 | 10.00 | 19.95 |
| HOP-92 | 5.70 | 2.26 | 6.30 | 7.94 | >100 |
| NCI-H226 | 14.60 | 4.00 | 6.30 | 15.84 | >100 |
| NCI-H23 | 6.87 | 16.5 | 19.95 | 15.84 | 12.58 |
| NCI-H322M | 23.00 | 19.1 | 0.05 | 0.08 | 19.95 |
| NCI-H460 | 4.19 | 10.4 | 5.01 | 6.30 | 1.00 |
| NCI-H522 | 6.55 | 4.89 | 1.00 | 6.30 | 39.81 |
| Colon cancer | |||||
| COLO 205 | 5.32 | 73.20 | 31.62 | 6.30 | nt |
| HCC-2998 | 13.00 | 26.60 | 79.34 | 10.00 | nt |
| HCT-116 | 3.76 | 4.04 | 5.01 | 7.94 | nt |
| HCT-15 | 2.47 | 17.00 | 3.16 | 5.01 | nt |
| KM12 | 3.98 | 32.30 | 63.09 | 7.94 | nt |
| SW-620 | 4.31 | 31.80 | 5.01 | 7.94 | nt |
| CNS cancer | |||||
| SF-268 | 7.13 | 6.62 | 19.95 | 7.94 | nt |
| SF-295 | 4.36 | 5.55 | 15.84 | 1.99 | nt |
| SF-539 | 2.86 | 2.29 | 12.58 | 10.00 | nt |
| SNB-19 | 6.00 | 6.80 | 3.98 | 12.58 | nt |
| SNB-75 | 2.06 | 1.58 | 12.58 | 6.30 | nt |
| U251 | 5.34 | 3.14 | 19.95 | 10.00 | 79.43 |
| Melanoma | |||||
| LOX IMVI | 7.05 | 13.50 | 5.01 | 7.94 | 6.30 |
| M14 | 2.23 | 16.50 | 6.30 | 5.01 | 50.11 |
| MDA-MB-435 | 1.15 | 22.80 | 15.84 | 3.16 | 10.00 |
| SK-MEL-2 | 2.82 | 15.20 | 12.58 | 12.58 | >100 |
| SK-MEL-28 | 6.69 | 11.40 | 31.62 | 0.31 | 50.11 |
| SK-MEL-5 | 2.85 | 6.38 | 15.84 | 3.98 | 12.58 |
| UACC-257 | 16.30 | 6.04 | 100 | 6.30 | >100 |
| UACC-62 | 2.92 | 6.29 | 1.25 | 5.01 | 12.58 |
| Ovarian cancer | |||||
| IGROV1 | 13.20 | 19.00 | 0.25 | 0.20 | 15.84 |
| OVCAR-3 | 4.23 | 7.86 | 3.16 | 5.01 | 25.11 |
| OVCAR-4 | 10.80 | 3.01 | 19.95 | 7.94 | 79.43 |
| OVCAR-5 | 9.38 | 14.80 | 19.95 | 10.00 | >100 |
| OVCAR-8 | 10.00 | 4.82 | 7.94 | 10.00 | 19.95 |
| NCI/ADR-RES | 3.59 | 8.37 | 6.30 | 12.58 | 39.81 |
| SK-OV-3 | 5.34 | 4.20 | 0.39 | 0.63 | >100 |
| Renal cancer | |||||
| 786-0 | 5.10 | 3.37 | 5.01 | 7.94 | 12.58 |
| A498 | 4.05 | 2.42 | 1.58 | 0.40 | 10.00 |
| ACHN | 8.09 | 3.15 | 0.15 | 0.20 | 10.00 |
| CAKI-1 | 5.46 | 11.30 | 0.10 | 0.16 | 5.01 |
| RXF 393 | 5.31 | 2.59 | 6.30 | 5.01 | 50.11 |
| SN12C | 8.10 | 16.90 | 6.3 | 6.30 | 25.11 |
| TK-10 | 11.00 | 2.63 | 0.10 | 0.10 | >100 |
| UO-31 | 5.90 | 3.75 | 1.99 | 1.25 | 5.01 |
| Prostate cancer | |||||
| PC-3 | 10.80 | 16.70 | 50.11 | 0.79 | 5.11 |
| DU-145 | 7.27 | 18.10 | 1.58 | 2.51 | 50.11 |
| Breast cancer | |||||
| MCF7 | 3.46 | 8.97 | 100 | 10.00 | 1.99 |
| MDA-MB-231/ATCC | 5.36 | 3.08 | 1.99 | 12.58 | >100 |
| HS 578T | 5.24 | 3.95 | 6.30 | 10.00 | >100 |
| BT-549 | 4.90 | 6.42 | 39.81 | 7.94 | 100 |
| T-47D | 5.52 | 2.16 | 3.16 | 6.30 | 79.43 |
| MDA-MB-468 | 2.35 | 7.22 | 0.20 | 0.01 | 31.62 |
nt: not tested.