Table 2.
Antitumor growth inhibitory activity (GI50/μM)a and cytotoxicity (LC50/μM)b data for compounds 3e and 3f in 5 dose studies against an NCI 60-cancer cell line panel.
| Panel/cell line | Compound 3e | Compound 3f | ||
|---|---|---|---|---|
| GI50 | LC50 | GI50 | LC50 | |
| Leukemia | 2.54 | 36.2 | 2.91 | >100 |
| CCRF-CEM | ||||
| HL-60(TB) | 1.85 | 21.0 | 2.67 | >100 |
| K-562 | 2.45 | 77.4 | 2.23 | >100 |
| MOLT-4 | 4.57 | >100 | 2.42 | >100 |
| RPMI-8226 | 1.19 | 65.9 | 3.25 | >100 |
| SR | 1.96 | 72.7 | 2.48 | >100 |
| Non-Small Cell Lung | 28.7 | >100 | 5.05 | >100 |
| A549/ATCC | ||||
| EKVX | 58.1 | >100 | >100 | >100 |
| HOP-62 | 8.78 | 51.2 | 1.99 | 33.0 |
| HOP-92 | 2.98 | 44.5 | 1.51 | 7.75 |
| NCI-H226 | 1.37 | 69.9 | 2.26 | >100 |
| NCI-H23 | 8.07 | 54.8 | 3.23 | 58.8 |
| NCI-H322M | 11.0 | >100 | 2.56 | >100 |
| NCI-H460 | 3.95 | 56.8 | 2.55 | >100 |
| NCI-H522 | 5.38 | >100 | 1.93 | >100 |
| Colon | 2.21 | 12.3 | 1.91 | nd |
| COLO 205 | ||||
| HCC-2998 | 6.95 | 47.2 | 2.99 | 4.71 |
| HCT-116 | 2.42 | 30.9 | 1.79 | 7.70 |
| HCT-15 | 19.8 | >100 | 2.27 | >100 |
| HT29 | 2.18 | 6.94 | 2.17 | nd |
| KM12 | 5.71 | 50.8 | 3.18 | >100 |
| SW-620 | 3.68 | 43.3 | 2.20 | >100 |
| CNS | 5.38 | 59.8 | 2.56 | >100 |
| SF-268 | ||||
| SF-295 | 4.96 | >100 | 2.36 | >100 |
| SF-539 | 1.73 | 6.94 | 1.54 | 5.56 |
| SNB-19 | 4.50 | 43.8 | 2.39 | 31.0 |
| SNB-75 | 1.58 | 18.6 | 1.46 | 5.47 |
| U251 | 3.01 | 66.2 | 1.81 | 7.72 |
| Melanoma | 1.97 | 9.37 | 1.89 | 8.66 |
| LOX IMVI | ||||
| MALME-3M | 3.30 | 73.8 | 1.70 | 8.33 |
| M14 | 4.46 | 47.8 | 1.90 | 7.25 |
| MDA-MB-435 | 4.97 | 68.6 | 1.93 | nd |
| SK-MEL-2 | 5.73 | >100 | 2.70 | >100 |
| SK-MEL-28 | 4.14 | 38.4 | 1.78 | 6.14 |
| SK-MEL-5 | 3.38 | 42.3 | 1.69 | 5.75 |
| UACC-257 | 12.9 | 66.9 | 17.9 | >100 |
| Ovarian | 20.0 | >100 | 5.91 | >100 |
| IGR-OV1 | ||||
| OVCAR-3 | 1.95 | 7.35 | 2.29 | 7.98 |
| OVCAR-4 | 2.41 | 25.2 | 2.18 | >100 |
| OVCAR-5 | 2.12 | 29.0 | 1.90 | 18.5 |
| OVCAR-8 | 10.1 | >100 | 3.45 | >100 |
| NCI/ADR-RES | >100 | >100 | 9.46 | >100 |
| SK-OV-3 | 11.9 | 49.9 | 1.98 | 8.68 |
| Renal | 6.15 | 46.2 | 1.75 | 5.85 |
| 786-0 | ||||
| A498 | 13.9 | 53.1 | 14.1 | 53.2 |
| ACHN | 11.8 | 59.0 | 1.76 | 6.14 |
| CAKI-1 | 68.1 | >100 | 35.1 | >100 |
| RXF 393 | 2.77 | 53.7 | 1.95 | 8.71 |
| SN12C | 6.07 | 76.3 | 1.74 | 8.59 |
| TK-10 | 6.84 | >100 | 3.16 | >100 |
| UO-31 | 7.95 | >100 | 3.20 | >100 |
| Prostate | 10.4 | 48.1 | 6.27 | >100 |
| PC-3 | ||||
| DU-145 | 82.1 | 68.8 | 2.25 | 14.8 |
| Breast | 2.25 | 48.1 | 2.45 | 77.8 |
| MCF7 | ||||
| MDA-MB-231/ATCC | 4.07 | 46.7 | 2.01 | 14.3 |
| HS 578T | 3.97 | >100 | 2.17 | >100 |
| BT-549 | 2.05 | >100 | 1.73 | >100 |
| T-47D | 1.68 | 13.1 | 1.50 | 5.74 |
| MDA-MB-468 | 1.69 | 6.90 | 1.63 | 6.78 |
a
GI50: 50% Growth inhibition, concentration of drug resulting in a 50% reduction in net protein increase compared with control cells.
b
LC50: Lethal concentration, concentration of drug lethal to 50% of cells.
nd: Not determined