Research Article
Synthesis, Characterisation, and In Vitro Anticancer Activity of Curcumin Analogues Bearing Pyrazole/Pyrimidine Ring Targeting EGFR Tyrosine Kinase
Table 2
Sixty human tumor cell lines anticancer screening data of curcumin analogues (1–14).
| Panel/cell line | Growth percent in one-dose assay | 1 | 2 | 3 | 5 | 6 | 8 | 10 | 11 | 12 | 13 |
| Leukemia | | | | | | | | | | | CCRF-CEM | −4.54 | 4.45 | 6.82 | 0.87 | 0.44 | 1.54 | −5.12 | 3.52 | 16.72 | 1.68 | HL-60(TB) | −24.28 | −20.94 | −21.36 | −28.92 | −28.17 | −30.36 | −42.20 | −23.89 | 61.33 | 3.67 | K-562 | 2.27 | −7.30 | 0.22 | −3.90 | 2.29 | −7.18 | −15.52 | 3.62 | 42.03 | 5.49 | MOLT-4 | −4.57 | −2.00 | −3.56 | −17.67 | 0.11 | −20.68 | −39.87 | −6.53 | 36.34 | 4.17 | RPMI-8226 | −22.31 | 2.91 | 3.32 | −11.32 | −14.46 | −16.73 | −33.60 | 14.25 | 62.49 | 2.88 | SR | −17.72 | 1.52 | 2.53 | 1.44 | −14.65 | −2.07 | −13.89 | −4.77 | 27.24 | −7.94 | Non-small-cell lung cancer | | | | | | | | | | | A549/ATCC | 8.75 | 4.03 | 12.02 | 5.90 | 4.71 | −3.98 | 8.40 | 41.73 | 71.68 | 10.09 | EKVX | 17.68 | 16.85 | 26.87 | −17.67 | 20.29 | −14.72 | −38.79 | 30.55 | 71.60 | 22.16 | HOP-62 | 8.39 | 17.06 | 30.22 | −7.78 | 11.62 | −35.66 | −67.73 | 43.53 | 70.77 | 4.85 | HOP-92 | −14.42 | −4.70 | −3.45 | NT | −15.38 | −27.02 | NT | NT | 33.70 | −21.24 | NCI-H226 | −3.72 | 5.73 | 15.88 | −4.32 | −0.89 | −3.70 | −8.19 | 38.48 | 76.20 | 11.70 | NCI-H23 | −25.82 | 3.16 | 10.74 | −12.87 | −10.41 | −26.09 | NT | 17.66 | 62.85 | −2.79 | NCI-H322M | NT | 22.13 | 27.32 | 12.63 | NT | 8.13 | −3.64 | 39.48 | NT | NT | NCI-H460 | 7.39 | 9.41 | 8.35 | 4.43 | 10.14 | 1.87 | −0.07 | 9.15 | 69.70 | 5.54 | NCI-H522 | −18.66 | −4.94 | −6.04 | 10.89 | −19.34 | 6.31 | −30.23 | 4.20 | 54.59 | −41.31 | Colon cancer | | | | | | | | | | | COLO 205 | −73.49 | 7.57 | 8.73 | 59.43 | −25.81 | −65.55 | −84.05 | 23.87 | 51.81 | −50.38 | HCC-2998 | 2.83 | 4.55 | 6.92 | 9.75 | 2.19 | 4.28 | 5.82 | 40.94 | 70.99 | 0.93 | HCT-116 | 1.16 | 4.61 | 4.95 | 2.15 | 1.60 | 1.48 | −5.83 | 6.90 | 34.75 | 0.33 | HCT-15 | 15.05 | 7.86 | 10.63 | 6.64 | 15.22 | 3.84 | −3.38 | 16.21 | 81.79 | 29.55 | HT29 | −34.95 | −11.07 | −41.84 | −33.57 | −22.35 | −38.54 | −52.39 | 0.38 | −6.41 | −76.24 | KM12 | 0.09 | 3.53 | 2.44 | 0.08 | −1.13 | −9.35 | −27.96 | 4.98 | 29.26 | −29.25 | SW-620 | 6.99 | 9.56 | 10.52 | 2.03 | 8.12 | −10.94 | −22.72 | 20.86 | 43.58 | 1.86 | CNS cancer | | | | | | | | | | | SF-268 | −6.38 | 13.87 | 20.12 | 6.57 | −11.50 | 3.80 | −12.52 | 27.97 | 48.19 | 3.56 | SF-295 | 2.83 | −21.89 | −21.61 | −55.32 | 0.53 | −51.02 | −71.47 | −29.68 | 92.76 | −5.25 | SF-539 | 4.06 | 0.16 | 3.68 | −16.58 | 5.95 | −19.58 | −39.79 | 4.02 | 69.02 | 11.95 | SNB-19 | 15.49 | 9.25 | 20.15 | 4.42 | 20.27 | 2.45 | 1.18 | 36.22 | 82.60 | 23.19 | SNB-75 | −4.71 | 18.75 | 26.93 | −12.60 | 9.53 | −30.53 | −53.18 | 27.28 | 44.32 | 5.50 | U251 | 2.33 | 4.31 | 13.38 | −1.59 | 6.19 | −12.27 | −1.47 | 35.06 | 55.64 | 2.97 | Melanoma | | | | | | | | | | | LOX IMVI | 1.22 | 3.04 | 4.00 | −20.87 | 1.89 | −29.79 | −37.11 | 9.29 | 49.04 | −16.09 | MALME-3M | 8.27 | 3.94 | 9.15 | −16.80 | 17.27 | −21.70 | −38.98 | 23.43 | 53.57 | −28.85 | M14 | 0.26 | 4.04 | 2.69 | −21.86 | 2.30 | −38.14 | −55.95 | 5.42 | 75.46 | −26.13 | MDA-MB-435 | 4.08 | 2.46 | −2.32 | −25.94 | −1.64 | −40.91 | −67.34 | −30.53 | 56.89 | −8.12 | SK-MEL-2 | −12.27 | −23.52 | −27.07 | −25.00 | −13.98 | −27.22 | −48.11 | −0.33 | 81.15 | −21.01 | SK-MEL-28 | 12.10 | 12.72 | 16.70 | 7.87 | 13.22 | 5.57 | −6.73 | 28.64 | 50.89 | 9.55 | SK-MEL-5 | −23.76 | −29.66 | −8.36 | −73.86 | 1.16 | −83.44 | −86.52 | −1.91 | 70.74 | −18.40 | UACC-257 | 1.28 | 3.11 | 13.66 | −15.89 | 4.80 | −21.42 | 16.03 | 87.13 | 62.46 | −1.90 | UACC-62 | 1.04 | 4.06 | 2.01 | −37.42 | 0.49 | −48.47 | −84.39 | 3.48 | 63.31 | −57.66 | Ovarian cancer | | | | | | | | | | | IGROV1 | −6.58 | 9.93 | 17.41 | 4.57 | 4.76 | −1.75 | −21.18 | 24.95 | 93.12 | 3.42 | OVCAR-3 | −26.77 | −10.97 | 3.89 | −26.44 | −34.15 | −37.33 | −46.92 | 12.55 | 59.34 | −7.57 | OVCAR-4 | 6.59 | 13.25 | 35.55 | 9.26 | 16.08 | 7.87 | 4.49 | 49.80 | 53.98 | 18.31 | OVCAR-5 | 13.18 | 10.94 | 31.32 | 0.88 | 20.53 | −4.24 | −7.74 | 84.49 | 101.67 | 5.83 | OVCAR-8 | 1.50 | −19.83 | 0.47 | −44.00 | −2.98 | −34.66 | −13.11 | 27.73 | 58.71 | 9.33 | NCI/ADR-RES | 20.83 | 17.46 | 27.91 | 12.01 | 20.50 | 7.64 | 3.18 | 28.13 | 90.66 | 39.32 | SK-OV-3 | −33.32 | −0.37 | −18.66 | −31.16 | −29.09 | −63.58 | −53.08 | 16.55 | 71.63 | −17.39 | Renal cancer | | | | | | | | | | | 786-0 | −14.80 | −2.20 | −6.90 | −32.92 | −1.18 | −59.07 | −76.67 | 9.91 | 82.57 | −58.93 | A498 | −11.83 | −0.60 | 31.49 | −13.65 | 12.02 | −14.70 | −25.17 | 56.41 | 62.76 | −56.92 | ACHN | 2.83 | 9.29 | 20.22 | 5.73 | 16.12 | 5.25 | 2.77 | 25.12 | 89.36 | 13.46 | CAKI-1 | 7.29 | 0.13 | −7.81 | −39.10 | 8.65 | −36.63 | −60.45 | −34.77 | 88.61 | 19.24 | RXF 393 | −50.32 | −53.60 | −43.84 | −57.61 | −47.46 | −67.29 | −70.03 | −3.83 | 23.75 | −63.92 | SN 12C | 14.20 | 9.00 | 17.95 | 2.06 | 18.30 | 0.47 | −3.11 | 14.23 | 62.26 | 22.14 | TK-10 | 16.15 | 23.10 | 38.12 | 24.04 | 28.55 | 15.86 | 6.18 | 65.02 | 102.74 | 21.38 | UO-31 | −34.84 | 2.71 | 14.05 | −16.95 | 0.97 | −38.74 | −44.64 | 23.86 | 54.25 | 3.16 | Prostate cancer | | | | | | | | | | | PC-3 | 6.54 | 4.24 | 9.01 | −14.26 | 8.08 | −10.82 | −33.14 | 12.92 | 61.01 | 12.99 | DU-145 | 1.23 | 11.66 | 6.77 | −11.84 | 2.20 | −26.64 | −45.74 | 28.87 | 80.37 | 13.04 | Breast cancer | | | | | | | | | | | MCF7 | 4.41 | 5.36 | 9.49 | 2.06 | 6.30 | −3.78 | −5.71 | 20.22 | 52.10 | 7.59 | MDA-MB-231/ATCC | 17.71 | 14.35 | 33.61 | 12.24 | 19.94 | 10.25 | 5.23 | 39.69 | 54.19 | 3.39 | HS 578T | −4.71 | 8.23 | 20.04 | −12.92 | −15.97 | −14.33 | −12.98 | 3.59 | 53.91 | −1.00 | BT-549 | −26.40 | −14.35 | −8.33 | −24.17 | −23.00 | −33.81 | −47.16 | 14.49 | 55.03 | −24.41 | T-47D | 4.55 | 18.50 | 31.15 | 2.29 | 5.65 | −22.55 | −23.93 | 48.99 | 59.14 | 1.57 | MDA-MB-468 | −24.19 | −26.40 | −14.60 | −27.56 | −29.14 | −30.34 | −31.86 | 2.97 | 6.34 | −35.04 |
| Mean | −4.66 | 1.81 | 7.23 | −12.25 | −0.66 | −19.19 | −28.71 | 19.03 | 59.94 | −5.46 |
| Range | 94.32 | 76.70 | 81.96 | 97.90 | 76.01 | 99.30 | 102.55 | 121.90 | 109.15 | 115.56 |
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NT: not tested.
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