Antitumor activity of pyrazolines 18a–q presented as growth inhibition percentages (GI%) using 59 subpanel tumor cell lines.
| Compound no. | PCEa | Cancer cell line assaysb (10.0 μM in one dose, GI%) | MGc% |
|---|---|---|---|
| 18a | 11/59 | Leukemia (HL-60(TB), 32%; K-562, 19%; MOLT-4, 32%; SR, 13%), non-small cell lung (A549/ATCC, 18%; EKVX, 11%; NCI-H226, 11%; NCI-H522, 18%), melanoma (MALME-3M, 11%; UACC-257, 14%), renal (UO-31, 12%) | 98.11 |
| 18b | 22/59 | Leukemia (HL-60(TB), 22%; K-562, 32%; MOLT-4, 17%; RPMI-8226, 11%), NSC lung (A549/ATCC, 13%; EKVX, 21%; HOP-62, 29%; NCI-H226, 15%; NCI-H522, 27%), colon (HCT-116, 26%; HT29, 13%), CNS (SNB-75, 13%), melanoma (UACC-62, 14%), ovarian (SK-OV-3, 26%), renal (CAKI-1, 18%; UO-31, 32%), prostate (PC-3, 22%), breast (MCF7, 13%; MDA-MB-231/ATCC, 11%; BT-549, 14%; T-47D, 31%; MDA-MB-468, 12%) | 92.03 |
| 18c | 21/59 | Leukemia (HL-60(TB), 46%; K-562, 33%; MOLT-4, 39%; RPMI-8226, 20%), NSC lung (A549/ATCC, 32%; EKVX, 15%; HOP-62, 26%; NCI-H522, 48%), colon (COLO 205, 22%; HT29, 19%), CNS (SNB-75, 14%; U251, 12%), melanoma (UACC-257, 32%), ovarian (OVCAR-8, 20%; SK-OV-3, 14%), renal (CAKI-1, 22%; UO-31, 20%), prostate (PC-3, 17%), breast (MCF7, 11%; BT-549, 14%; T-47D, 24%) | 90.58 |
| 18d | 18/59 | Leukemia (HL-60(TB), 57%; K-562, 32%; MOLT-4, 37%), non-small cell lung (A549/ATCC, 24%; EKVX, 16%; HOP-62, 29%; NCI-H322M, 14%; NCI-H522, 43%), colon (HT29, 14%), CNS (U-251, 17%), melanoma (UACC-257, 37%), ovarian (OVCAR-8, 15%; SK-OV-3, 13%), renal (CAKI-1, 14%; TK-10, 12%; UO-31, 27%), breast (BT-549, 15%; T-47D, 17%) | 93.02 |
| 18e | 15/59 | Leukemia (HL-60(TB), 48%; K-562, 29%; MOLT-4, 35%; RPMI-8226, 12%), non-small cell lung (EKVX, 12%; HOP-62, 14%; NCI-H226, 12%; NCI-H522, 15%), colon (HCT-116, 17%), CNS (SNB-75, 18%), renal (CAKI-1, 17%; UO-31, 22%), prostate (PC-3, 15%), (MCF7, 13%; T-47D, 17%) | 94.18 |
| 18f | 21/59 | Leukemia (HL-60(TB), 14%; MOLT-4, 30%; RPMI-8226, 18%), NSC lung (A549/ATCC, 16%; EKVX, 13%; HOP-62, 12%; NCI-H226, 17%; NCI-H522, 37%), colon (HCT-116, 20%; HT29, 12%), CNS (SNB-75, 20%; U251, 11%), melanoma (SK-MEL-2, 11%; UACC-257, 26%; UACC-62, 12%), renal (CAKI-1, 16%; UO-31, 24%), prostate (PC-3, 28%), breast (MCF7, 11%; T-47D, 16%; MDA-MB-468, 15%) | 93.80 |
| 18g | 48/59 | Leukemia (HL-60(TB), 66%; K-562, 80%; MOLT-4, 56%; SR, 50%), NSC lung (A549/ATCC, 43%; EKVX, 25%; HOP-62, 26%; NCI-H23, 12%; NCI-H322M, 12%; NCI-H460, 17%; NCI-H522, 73%), colon (COLO 205, 33%; HCT-116, 37%; HCT-15, 45%; HT29, 15%; KM12, 37%; SW-620, 25%), CNS (SF-268, 11%; SF-295, 30%; SNB-19, 13%; SNB-75, 30%; U251, 23%), melanoma (LOX IMVI, 16%; MALME-3M, 14%; M14, 32%; MDA-MB-435, 76%; SK-MEL-2, 33%; SK-MEL-28, 23%; SK-MEL-5, 38%; UACC-257, 40%; UACC-62, 36%), ovarian (IGROV1, 23%; OVCAR-3, 24%; OVCAR-4, 22%; NCI/ADR-RES, 38%; SK-OV-3, 26%), renal (786-0, 22%; A498, 16%; ACHN, 12%; CAKI-1, 43%; UO-31, 26%), prostate (PC-3, 33%), breast (MCF7, 52%; MDA-MB-231/ATCC, 14%; HS 578T, 15%; BT-549, 27%; T-47D, 32%; MDA-MB-468, 45%) | 72.98 |
| 18h | 51/59 | Leukemia (CCRF-CEM, 41%; HL-60(TB), 73%; K-562, 55%; MOLT-4, 62%; RPMI-8226, 16%; SR, 30%), NSC lung (A549/ATCC, 45%; EKVX, 41%; HOP-62, 47%; NCI-H226, 15%; NCI-H23, 12%; NCI-H322M, 48%; NCI-H460, 54%; NCI-H522, 55%), colon (COLO 205, 20%; HCT-116, 35%; HCT-15, 56%; HT29, 20%; KM12, 21%), CNS (SF-268, 39%; SF-295, 23%; SNB-19, 17%; U251, 48%), melanoma (LOX IMVI, 34%; MALME-3M, 21%; M14, 29%; SK-MEL-2, 28%; SK-MEL-28, 11%; SK-MEL-5, 38%; UACC-257, 39%; UACC-62, 12%), ovarian (IGROV1, 28%; OVCAR-3, 35%; OVCAR-4, 22%; OVCAR-8, 41%; NCI/ADR-RES, 22%; SK-OV-3, 25%), renal (786-0, 33%; ACHN, 25%; CAKI-1, 33%; RXF 393, 29%; SN12C, 17%; TK-10, 25%; UO-31, 47%), prostate (PC-3, 21%; DU-145, 19%), breast (MCF7, 22%; MDA-MB-231/ATCC, 32%; BT-549, 19%; T-47D, 30%; MDA-MB-468, 17%) | 72.20 |
| 18i | 12/59 | Leukemia (HL-60(TB), 46%; MOLT-4, 28%), non-small cell lung (A549/ATCC, 35%; EKVX, 12%; HOP-62, 20%; NCI-H226, 13%; NCI-H522, 29%), colon (HT-29, 17%), melanoma (UACC-257, 36%), renal (CAKI-1, 23%; UO-31, 28%), breast (T-47D, 17%) | 96.46 |
| 18j | 10/59 | Leukemia (HL-60(TB), 35%; K-562, 13%; MOLT-4, 26%), non-small cell lung (A549/ATCC, 24%; EKVX, 12%; NCI-H226, 11%; NCI-H522, 14%), CNS (SNB-75, 12%), melanoma (UACC-257, 14%), breast (T-47D, 16%) | 97.16 |
| 18k | 12/59 | Leukemia (HL-60(TB), 18%; MOLT-4, 27%; RPMI-8226, 11%), non-small cell lung (A549/ATCC, 13%; NCI-H226, 14%; NCI-H522, 35%), colon (HT-29, 20%), CNS (SNB-75, 11%), melanoma (K-MEL-5, 14%), renal (UO-31, 15%), prostate (PC-3, 21%), breast (MDA-MB-468, 16%) | 97.49 |
| 18l | 14/59 | Leukemia (HL-60(TB), 47%; K-562, 18%; MOLT-4, 33%), non-small cell lung (A549/ATCC, 40%; HOP-62, 11%; NCI-H522, 34%), colon (HT-29, 19%), CNS (SNB-75, 11%), melanoma (UACC-257, 45%), renal (CAKI-1, 14%; UO-31, 16%), breast (MCF7, 11%; BT-549, 13%; T-47D, 11%) | 95.78 |
| 18m | 18/59 | Leukemia (HL-60(TB), 63%; K-562, 40%; MOLT-4, 48%), NSC lung (A549/ATCC, 20%; HOP-62, 17%; NCI-H226, 11%; NCI-H522, 13%), colon (COLO 205, 19%; HCT-116, 18%; HCT-15, 14%), CNS (SNB-75, 12%), ovarian (SK-OV-3, 16%), renal (A498, 14%; UO-31, 34%), prostate (PC-3, 15%), breast (MCF7, 16%; BT-549, 14%; T-47D, 22%) | 91.96 |
| 18n | 20/59 | Leukemia (HL-60(TB), 55%; K-562, 26%; MOLT-4, 38%), NSC lung (EKVX, 28%; HOP-62, 20%; NCI-H226, 14%; NCI-H522, 20%), colon (HCT-116, 18%; KM12, 12%), CNS (SNB-75, 15%), melanoma (SK-MEL-2, 18%; SK-MEL-5, 21%), ovarian (OVCAR-4, 12%), renal (CAKI-1, 15%; UO-31, 24%), prostate (PC-3, 15%), breast (MCF7, 65%; MDA-MB-231/ATCC, 12%; T-47D, 14%; MDA-MB-468, 36%) | 93.24 |
| 18o | 15/59 | Leukemia (HL-60(TB), 51%; K-562, 32%; MOLT-4, 40%; SR, 11%), NSC lung (A549/ATCC, 31%; HOP-62, 18%; NCI-H522, 43%), colon (HT29, 17%), CNS (SNB-75, 15%), melanoma (SK-MEL-5, 12%; UACC-257, 38%), renal (CAKI-1, 12%; UO-31, 19%), breast (BT-549, 11%; T-47D, 18%) | 94.17 |
| 18p | 11/59 | Leukemia (HL-60(TB), 31%; K-562, 23%), NSC lung (HOP-62, 26%; NCI-H226, 15%; NCI-H522, 13%), colon (HCT-116, 17%), CNS (SF-268, 11%), ovarian (SK-OV-3, 16%), renal (UO-31, 25%), breast (T-47D, 25%; MDA-MB-468, 13%) | 97.33 |
| 18q | 6/59 | CNS (SNB-75, 13%), renal (A498, 13%; CAKI-1, 13%; UO-31, 24%), breast (MCF7, 12%; MDA-MB-468, 12%) | 97.51 |
| Imatinib | 20/59 | Leukemia (MOLT-4, 18%; PRMI-8226, 12.6%; SR, 14.6%), NSC lung (EKVX, 15.7%; NCI-H226, 10.6%; NCI-H23, 17.1%), colon (HCT-116, 18.6%; HCT-15, 11.5%; HT-29, 47.1%), CNS (SF-295, 15.1%; SF-539, 24.5%; U251, 10.6%), melanoma (LOX IMVI, 11.6%; SK-MEL-5, 22.3%), renal (A-498, 13.7%), prostate (PC-3, 10.6%; DU-145, 14.4%), breast (MDA-MB-231/ATCC, 11.2%; T-47D, 18.6%; MDA-MB-468, 29.1%) | 92.62% |
a
PCE: positive cytotoxic effect; the ratio between the number of cell lines with percentage growth inhibition >10% and the total cell lines.
b
MGI%: mean growth inhibition percent.
c
MG%: mean growth percent.