Table 5.
In vitro growth inhibition % (GI %) of target 2,5-diarylbenzimidazole 8a-u against NCI panel of 60 tumor cell lines at 10 µM concentration
| Cell name | GI% | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 8a | 8b | 8c | 8d | 8e | 8f | 8g | 8h | 8i | 8j | 8k | 8l | 8m | 8n | 8o | 8p | 8q | 8r | 8s | 8t | 8u | |
| Leukemia | |||||||||||||||||||||
| CCRF-CEM | 88.16 | 54.37 | 44.52 | La | 35.93 | 80.48 | 61.96 | 94.27 | 80.82 | 35.00 | L | 89.42 | 45.90 | 38.76 | L | 71.92 | 46.97 | L | L | 56.12 | L |
| HL-60(TB) | 95.58 | 14.38 | 38.07 | 90.03 | 24.68 | 36.28 | 17.05 | 82.91 | 55.15 | 30.37 | L | 52.20 | 18.79 | – | 47.15 | – | 50.70 | L | 45.32 | 12.89 | 67.85 |
| K-562 | 78.58 | 21.43 | 41.67 | 60.91 | 26.24 | 63.00 | 30.39 | 99.48 | 60.56 | 88.06 | L | 48.52 | 22.75 | 23.67 | 85.46 | 49.86 | 98.12 | L | 50.30 | 52.90 | L |
| MOLT-4 | 89.54 | 31.49 | 35.43 | 65.79 | 36.14 | 49.49 | 21.20 | 88.52 | 78.97 | 59.41 | L | 78.57 | 35.76 | 22.13 | 60.79 | 68.62 | 71.63 | L | 83.69 | 58.90 | 96.04 |
| RPMI-8226 | 88.59 | 9.59 | 81.63 | 98.47 | 23.38 | 81.35 | 86.93 | 96.71 | 24.77 | L | L | 32.41 | 76.82 | 44.49 | 88.15 | 56.71 | L | L | L | 62.25 | L |
| SR | 92.31 | 36.75 | 36.30 | 77.01 | 44.12 | 36.30 | 17.59 | 85.9 | 81.89 | 92.65 | L | 72.20 | 28.49 | 26.93 | 75.20 | 26.42 | L | L | 77.15 | 31.36 | L |
| Non-small cell lung cancer | |||||||||||||||||||||
| A549/ATCC | L | –b | 20.15 | 79.76 | – | 17.21 | 29.27 | L | 11.15 | L | 76.72 | 5.94 | 13.69 | – | 86.99 | 7.53 | L | L | 7.66 | 8.76 | 70.84 |
| EKVX | 96.49 | 13.81 | 41.83 | 87.59 | 19.18 | 22.69 | 12.24 | 92.19 | 23.40 | L | 98.06 | 12.95 | 10.58 | – | 67.24 | 7.59 | L | L | 37.02 | 42.46 | 90.75 |
| HOP-62 | L | 19.26 | 15.41 | ndc | 21.42 | nd | nd | L | 41.98 | L | L | 55.53 | 19.45 | 14.62 | ndc | 32.45 | L | L | nd | 18.43 | L |
| HOP-92 | L | – | – | 68.37 | 6.30 | 7.10 | – | L | 27.01 | L | 70.36 | 17.43 | – | – | L | 6.79 | L | L | – | 36.64 | L |
| NCI-H226 | 93.32 | – | 19.33 | L | 11.44 | 49.54 | 50.35 | L | 7.75 | 98.27 | 82.17 | 24.51 | – | 22.33 | 88.60 | 30.08 | L | L | 37.63 | 35.69 | L |
| NCI-H23 | 83.12 | – | 9.68 | L | – | 46.67 | 49.43 | 94.63 | 6.56 | L | L | 23.97 | – | 10.75 | L | 56.65 | L | L | 29.22 | 33.93 | L |
| NCI-H322M | 94.14 | – | 6.09 | 88.01 | – | 12.31 | 15.67 | 96.71 | 18.26 | L | 95.89 | 24.04 | – | – | 70.15 | – | L | L | 18.15 | 28.86 | 96.14 |
| NCI-H460 | L | – | 13.08 | 86.38 | – | 15.82 | 56.31 | L | 5.05 | L | L | 14.98 | – | – | L | 56.63 | L | L | 63.79 | 17.46 | L |
| NCI-H522 | L | 38.06 | 25.96 | L | 29.39 | 37.77 | 50.69 | L | 43.41 | 89.70 | L | 38.23 | 21.28 | 96.2 | L | 55.77 | L | L | 30.91 | 40.86 | L |
| Colon cancer | |||||||||||||||||||||
| COLO 205 | L | – | 32.62 | nd | 35.42 | nd | nd | L | 32.41 | L | L | 76.84 | – | 33.71 | nd | 34.57 | L | L | nd | 18.27 | L |
| HCC-2998 | 73.20 | – | – | 98.55 | – | 8.92 | 44.26 | 99.64 | 14.86 | 88.46 | L | 15.01 | – | – | 77.99 | 15.94 | 79.58 | L | 86.84 | 14.58 | L |
| HCT-116 | L | – | 12.67 | 97.43 | 15.03 | 52.52 | 41.62 | L | 42.79 | L | L | 43.83 | 22.29 | 23.4 | 98.39 | 37.67 | L | L | 69.55 | 43.08 | L |
| HCT-15 | 94.00 | – | 27.47 | 71.57 | – | 65.20 | 38.39 | L | 5.17 | 79.23 | 78.11 | – | 13.68 | – | L | – | 63.00 | 95.20 | 23.27 | 58.25 | 44.27 |
| HT29 | L | 16.35 | 33.92 | 84.54 | 95.82 | 14.69 | 47.26 | L | 74.50 | L | L | L | 25.35 | nd | L | 19.88 | L | L | L | 20.28 | L |
| KM12 | 84.00 | 19.80 | 25.98 | L | 21.86 | 30.49 | 36.44 | L | 38.72 | L | L | 34.46 | 11.66 | 13.78 | 85.44 | 62.74 | L | L | 68.41 | 23.33 | L |
| SW-620 | 77.39 | – | – | 70.84 | – | 30.32 | 37.93 | L | 6.72 | L | 98.83 | 21.77 | – | – | L | 6.31 | L | L | 69.62 | 7.98 | L |
| CNS cancer | |||||||||||||||||||||
| SF-268 | L | 16.82 | 15.05 | 99.03 | 16.00 | 36.62 | 31.99 | L | 37.35 | 84.67 | L | 40.44 | 9.02 | 21 | L | 24.23 | L | L | 72.71 | 43.02 | L |
| SF-295 | L | – | 18.50 | 83.16 | 10.86 | 31.38 | 54.12 | L | 21.96 | 167.36 | 96.39 | 50.95 | 19.91 | 29.8 | L | 11.79 | L | L | 84.96 | 51.90 | L |
| SF-539 | L | 13.68 | 28.61 | L | 32.21 | 36.88 | 49.79 | L | 53.27 | 34.15 | L | 42.58 | 32.57 | 24.35 | L | 32.42 | L | L | 47.21 | 45.33 | L |
| SNB-19 | 95.02 | – | – | 90.36 | – | 21.40 | 25.17 | L | 15.85 | L | L | 16.06 | – | 36.2 | L | nd | L | L | 39.72 | 45.69 | L |
| SNB-75 | L | 6.56 | 11.00 | 99.21 | – | – | – | 95.58 | 17.83 | L | 90.95 | 25.75 | – | – | L | 7.89 | L | L | 6.41 | 27.17 | L |
| U251 | L | – | 14.27 | 99.86 | 14.62 | 20.71 | 42.32 | L | 32.10 | L | 97.28 | 44.79 | 9.71 | 15.28 | L | 75.53 | L | L | 75.23 | 25.71 | L |
| Melanoma | |||||||||||||||||||||
| LOX IMVI | 88.38 | 7.43 | – | 92.90 | – | 62.46 | 56.54 | 98.7 | 26.07 | L | L | 37.90 | 18.79 | 7.53 | L | 14.74 | L | L | 44.94 | 34.64 | L |
| MALME-3 M | 99.32 | 39.71 | 47.13 | L | 78.42 | 40.49 | 73.63 | L | L | L | L | 87.59 | 18.33 | 76.79 | L | 58.88 | L | L | L | 18.37 | L |
| M14 | 81.80 | – | 8.28 | L | 19.74 | 34.40 | 43.27 | L | 39.14 | 70.41 | 90.97 | 63.49 | – | 40.28 | 90.88 | 25.37 | L | L | 42.14 | 30.86 | L |
| MDA-MB-435 | 63.10 | 5.45 | 18.89 | 74.61 | 30.39 | 73.65 | 48.54 | L | 63.84 | 76.54 | 76.03 | 26.54 | – | 24.97 | L | 15.16 | 98.89 | L | 89.90 | 14.33 | L |
| SK-MEL-2 | 60.21 | – | 19.50 | 34.31 | 8.51 | 16.71 | 21.79 | nd | 37.55 | 80.99 | 39.06 | 25.77 | 11.11 | nd | L | 23.97 | L | L | 76.06 | – | L |
| SK-MEL-28 | 82.67 | – | 20.43 | 96.19 | 28.87 | 29.06 | 40.41 | L | 52.90 | 64.23 | L | 52.45 | 5.70 | 31.45 | 78.18 | 15.97 | L | L | 70.75 | 14.62 | L |
| SK-MEL-5 | 85.73 | 10.91 | 39.03 | L | 39.52 | 67.75 | 89.35 | L | 40.51 | L | L | 55.34 | 22.29 | 42.62 | L | 69.47 | L | L | 53.32 | 68.78 | L |
| UACC-257 | 88.80 | – | 14.61 | L | 13.76 | – | 54.30 | 85.05 | 47.38 | 57.67 | L | 52.86 | 14.32 | 25.57 | 42.37 | – | L | L | 24.65 | – | L |
| UACC-62 | 75.88 | – | 14.66 | 99.46 | 18.69 | 35.47 | 70.39 | L | 50.84 | 58.87 | 98.01 | 47.57 | 6.39 | 68.48 | 95.30 | 19.57 | L | L | 37.51 | 24.28 | L |
| Ovarian cancer | |||||||||||||||||||||
| IGROV1 | 82.83 | 12.96 | 10.09 | 79.92 | 21.96 | 10.98 | 16.96 | L | 11.20 | L | 84.81 | 20.28 | – | – | 84.28 | 5.71 | L | L | – | 7.82 | 92.38 |
| OVCAR-3 | L | 11.09 | 7.38 | L | 7.25 | 12.52 | 29.45 | L | 8.04 | L | L | 37.61 | – | – | L | – | L | L | 47.55 | 10.78 | L |
| OVCAR-4 | 94.42 | 12.43 | 20.07 | L | – | 37.84 | 21.95 | L | 27.06 | L | 86.01 | 9.88 | 8.31 | – | L | 15.65 | L | L | 20.81 | 38.89 | L |
| OVCAR-5 | 77.04 | – | – | 63.24 | – | – | – | L | – | 91.17 | 69.48 | – | – | – | 55.93 | – | L | L | – | – | 37.36 |
| OVCAR-8 | L | 10.32 | 24.52 | L | 25.20 | 52.57 | 48.68 | L | 38.12 | L | L | 28.08 | 23.61 | 15.01 | L | 19.01 | L | L | 43.17 | 17.17 | L |
| NCI/ADR-RES | 63.15 | – | 6.59 | 47.95 | – | 24.51 | – | 63.2 | – | 31.99 | 28.06 | – | – | – | 56.35 | – | 23.04 | 49.30 | – | 11.23 | 24.32 |
| SK-OV-3 | L | 25.63 | 63.95 | nd | 56.26 | nd | nd | L | 53.95 | 68.31 | L | – | – | 20.23 | nd | 36.21 | L | L | nd | 15.10 | L |
| Renal cancer | |||||||||||||||||||||
| 786–0 | 91.76 | 5.43 | 21.32 | 86.04 | 16.58 | 18.59 | 27.80 | L | 23.41 | L | L | 18.10 | 29.04 | – | L | 22.17 | L | L | 52.04 | 26.55 | L |
| A498 | – | – | – | – | – | – | – | 54.5 | – | – | – | – | – | – | 53.91 | 10.17 | L | L | – | 56.16 | L |
| ACHN | L | – | – | 83.27 | – | 36.51 | 33.83 | L | – | L | 87.70 | – | 8.59 | 9.17 | 94.16 | – | L | L | – | 53.09 | 69.94 |
| CAKI-1 | L | 9.41 | 10.00 | 91.59 | 17.64 | 41.47 | 49.73 | L | 5.16 | 85.29 | 84.62 | – | – | 23.76 | L | – | L | L | 18.49 | 38.36 | 97.13 |
| RXF 393 | L | – | 29.22 | 85.95 | – | 49.96 | 30.81 | L | 14.49 | L | L | 37.22 | 15.21 | 20.09 | L | 31.57 | L | L | 69.12 | 96.54 | L |
| SN12C | nd | nd | nd | 91.53 | nd | 35.21 | 32.21 | L | nd | nd | nd | 26.96 | nd | 9.66 | 59.42 | nd | nd | nd | 31.33 | nd | nd |
| TK-10 | 65.04 | – | – | 50.64 | – | 18.99 | 6.66 | L | – | L | 40.00 | – | – | – | 95.02 | – | L | L | – | 10.93 | 62.64 |
| UO-31 | 86.22 | 21.59 | 30.63 | 98.53 | 38.19 | 54.04 | 45.55 | L | 10.49 | 98.91 | 83.20 | 9.13 | 9.12 | 21.84 | L | 14.89 | 81.69 | L | 8.70 | 31.95 | 41.11 |
| Prostate cancer | |||||||||||||||||||||
| PC-3 | 90.74 | 11.75 | 24.64 | 82.18 | 11.47 | 55.54 | 37.87 | L | 34.39 | L | 87.92 | 51.22 | 13.61 | 12.94 | 78.51 | 48.79 | L | L | 56.49 | 58.53 | L |
| DU-145 | L | – | 18.43 | 79.68 | – | 18.43 | 17.07 | L | 13.98 | L | 85.12 | 27.88 | – | – | L | – | L | L | 16.20 | 51.99 | L |
| Breast cancer | |||||||||||||||||||||
| MCF7 | 96.94 | 43.15 | 50.96 | 98.08 | 70.45 | 54.14 | 85.99 | L | 88.20 | L | L | 77.80 | 20.64 | 73.09 | 93.74 | 72.33 | L | L | 84.87 | 48.06 | L |
| MDA-MB-231/ATCC | 88.16 | 14.06 | – | 94.36 | – | 38.00 | 30.48 | 98.72 | 22.38 | L | 97.65 | 26.37 | 14.33 | 7.37 | L | 45.17 | L | L | 75.12 | 89.71 | L |
| HS 578 T | L | – | 19.99 | 92.89 | 6.89 | 49.91 | 51.04 | L | 52.61 | L | 89.32 | 46.23 | – | 37.73 | L | 27.07 | L | L | 86.87 | 48.77 | L |
| BT-549 | L | – | – | 96.59 | – | 38.19 | 35.43 | L | 32.71 | 29.81 | L | 10.40 | 17.16 | – | 60.58 | – | 6.97 | L | 42.90 | 25.73 | L |
| T-47D | 93.65 | 50.90 | 69.11 | nd | 39.30 | nd | nd | L | 86.79 | L | 94.97 | 52.49 | 40.60 | 38.08 | nd | 79.76 | L | L | nd | 61.77 | L |
| MDA-MB-468 | 99.81 | 18.93 | 22.71 | L | 7.65 | 24.73 | 39.16 | L | 54.60 | L | L | 44.35 | 16.21 | – | L | 65.77 | L | L | 88.69 | 30.39 | L |
| Mean growth inhibition % | 97.73 | 8.49 | 20.74 | 92.51 | 16.75 | 33.74 | 36 | L | 33.08 | L | L | 34.39 | 10.90 | 13.64 | L | 25.43 | L | L | 49.49 | 33.49 | L |
aGI% > 100; bGI% < 5%; cnot detected