JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
1525
Table 1. Antitumor activity of the designed hydrazones at 10 mM concentration.
0 cell lines assay in one dose 10.0 mM concentration (GI%)
Most sensitive cell lines
Leukaemia (HL-60 (TB): 60.3, K-562: 11.3, MOLT-4: 25.5), NSC Lung Cancer (A549/ATCC: 28.5, HOP-62: 12.0, NCI-H522: 42.1), CNS Cancer
U251: 20.4), Melanoma (SK-MEL-2: 21.5, UACC-257: 44.2), Ovarian Cancer (OVCAR-8: 15.1).
Leukaemia (CCRF-CEM: 11.1, HL-60(TB): 20.5, K-562: 18.8), NSC Lung Cancer (A549/ATCC: 10.6, HOP-62: 16.5, NCI-H226: 11.9, NCI-H522:
5.1), Colon Cancer (HT29: 13.3), Ovarian Cancer (SK-OV-3: 16.9), Renal Cancer (A498: 11.2, UO-31: 16.3), Prostate Cancer (PC-3: 17.9),
a
6
b
Compd No
PCE
4
10/59
(
5
13/59
1
Breast Cancer (T-47D: 13.7).
6
52/59
Leukaemia (CCRF-CEM: 22.4, HL-60(TB): 62.5, K-562: 72.2, MOLT-4: 53.2, PRMI-8226: 12.3, SR: 67.5), NSC Lung Cancer (A549/ATCC: 58.7,
EKVX: 12.6,HOP-62: 25.1, NCI-H226: 16.3, NCI-H23: 10.4, NCI-H460: 33.2, NCI-H522: 95.5), Colon Cancer (COLO 205: 14.3, HCC-2998: 15.5,
HCT-116: 38.2, HCT-15: 50.2, HT29: 50.5, KM12: 49.2, SW-620: 63.8), CNS Cancer (SF-268: 14.3, SF-295: 24.0, SF-539: 10.7, SNB-19: 20.2,
SNB-75: 10.3, U251: 23.7), Melanoma (LOX IMVI: 27.6, MALME-3M: 30.3 , M14: 33.2, MDA-MB-435: 82.9, SK-MEL-2: 52.3, SK-MEL-28: 10.6,
SK-MEL-5: 32.8, UACC-257: 58.9, UACC-62: 38.4), Ovarian Cancer (IGROV1: 36.8, OVCAR-3: 32.2, OVCAR-8: 16.2, NCI/ADR-RES: 26.5, SK-
OV-3: 21.9), Renal Cancer (A498: 30.9, CAKI-1: 32.8, SN12C: 12.6, TK-10: 14.9, UO-31: 21.5), Prostate Cancer (PC-3: 21.2, DU-145: 11.2),
Breast Cancer (MCF7: 55.1, HS 578 T: 14.9, BT-549: 12.4, T-47D: 14.7, MDA-MB-468: 25.8).
7
8
9
7/59
9/59
Leukaemia (HL-60 (TB): 52.1, K-562: 14.0, MOLT-4: 29.4), NSC Lung Cancer (NCI-H522: 15.7), Melanoma (SK-MEL-2: 12.8), Renal Cancer
(A498: 12.3), Prostate Cancer (PC-3: 22.8).
Leukaemia (CCRF-CEM: 11.8, HL-60(TB): 23.1, K-562: 13.6, MOLT-4: 23.9, SR: 20.2), NSC Lung Cancer ( A549/ATCC: 11.1, NCI-H522: 15.9),
Colon Cancer (HCT-116: 10.8), Melanoma (UACC-257: 18.4).
Leukaemia (CCRF-CEM: 20.8, HL-60(TB): 24.3, K-562: 44.1, MOLT-4: 22.6, SR: 43.8), NSC Lung Cancer (A549/ATCC: 12.7, NCI-H522: 53.9),
Colon Cancer (HCT-116: 13.9, HCT-15: 16.3, HT29: 17.7, KM12: 25.1, SW-620: 15.2), CNS Cancer (U251: 13.7), Melanoma (MALME-3M:
27/59
1
1
5.2 , MDA-MB-435: 47.5, SK-MEL-2: 19.8, SK-MEL-5: 13.5, UACC-257: 28.4, UACC-62: 19.1), Ovarian Cancer (IGROV1: 12.3, NCI/ADR-RES:
4.6), Renal Cancer (A498: 17.9, CAKI-1: 25.0, UO-31: 12.3), Prostate Cancer (PC-3: 26.9), Breast Cancer (MCF7: 21.4, MDA-MB-468: 21.5)
1
0
11/59
Leukaemia (CCRF-CEM: 10.6, HL-60(TB): 42.9, MOLT-4: 21.1), NSC Lung Cancer (A549/ATCC: 29.8 , NCI-H226: 13.4, NCI-H522: 20.8), Colon
Cancer (HT29: 10.8), Melanoma (SK-MEL-2: 11.8, UACC-257: 29.0), Ovarian Cancer (OVCAR-8: 11.3), Prostate Cancer (PC-3: 13.8).
Leukaemia (HL-60(TB): 50.5, K-562: 26.2, MOLT-4: 32.5), NSC Lung Cancer (NCI-H522: 11.7), Prostate Cancer (PC-3: 10.9).
Leukaemia (HL-60(TB): 38.0, K-562: 17.2, MOLT-4: 29.8), NSC Lung Cancer (A549/ATCC: 28.4, HOP-62: 11.4, NCI-H522: 40.4), Colon Cancer
1
1
1
2
5/59
9/59
(
HT29: 20.5), Melanoma (UACC-257: 39.2), Renal Cancer (UO-31: 11.2).
1
3
4
10/59
12/59
Leukaemia (HL-60(TB): 47.7, K-562: 32.5, MOLT-4: 32.3), NSC Lung Cancer (A549/ATCC: 21.6, HOP-62: 12.7), CNS Cancer (SNB-75: 15.1),
Melanoma ( UACC-257: 35.5), Ovarian Cancer (SK-OV-3: 11.7), Renal Cancer (UO-31: 15.7), Breast Cancer (T-47D: 12.5)
Leukaemia (HL-60(TB): 36.0, K-562: 25.7, MOLT-4: 26.4, SR: 49.2), NSC Lung Cancer (A549/ATCC: 29.3, HOP-62: 15.8, NCI-H522: 26.0), Colon
Cancer (HT29: 18.6), Melanoma ( UACC-257: 42.4), Ovarian Cancer (OVCAR-8: 14.5), Renal Cancer ( CAKI-1: 11.7), Breast Cancer (T-
1
4
7D: 11.8).
1
5
6
14/59
59/59
Leukaemia (CCRF-CEM: 16.1, HL-60(TB): 36.5, K-562: 23.4, MOLT-4: 11.6, SR: 15.6), NSC Lung Cancer (A549/ATCC: 11.9, HOP-62: 18.9, NCI-
H226: 10.3), Colon Cancer (HCT-116: 10.7), Melanoma (UACC-257: 10.1), Ovarian Cancer (SK-OV-3: 17.1), Renal Cancer (UO-31: 14.4),
Prostate Cancer (PC-3: 19.1), Breast Cancer (T-47D: 18.2)
Leukaemia (CCRF-CEM: 84.7, HL-60(TB): 93.7, K-562: 59.5, MOLT-4: 90.8, PRMI-8226: 51.3, SR: 79.6), NSC Lung Cancer (A549/ATCC: 61.2,
EKVX: 74.2,HOP-62: 71.8, NCI-H226: 44.8, NCI-H23: 45.2, NCI-H322M: 61.6, NCI-H460: 85.9, NCI-H522: 84.9), Colon Cancer (COLO 205:
1
68.8, HCC-2998: 52.7, HCT-116: 70.9, HCT-15: 82.0, HT29: 56.4, KM12: 65.9, SW-620: 56.7), CNS Cancer (SF-268: 61.6, SF-295: 62.0, SF-
539: 44.7, SNB-19: 54.6, SNB-75: 22.3, U251: 72.2), Melanoma (LOX IMVI: 78.6, MALME-3M: 36.5 , M14: 67.5, MDA-MB-435: 40.3, SK-MEL-
2: 60.0, SK-MEL-28: 44.1, SK-MEL-5: 67.8, UACC-257: 77.4, UACC-62: 83.6), Ovarian Cancer (IGROV1: 59.0, OVCAR-3: 77.2, OVCAR-4: 56.3,
OVCAR-5: 35.3, OVCAR-8: 72.1, NCI/ADR-RES: 70.1, SK-OV-3: 60.1), Renal Cancer (786-0: 67.0, A498: 24.8, ACHN: 71.7, CAKI-1: 65.1, RXF
93: 47.0, SN12C: 41.4, TK-10: 54.2, UO-31: 82.0), Prostate Cancer (PC-3: 45.7, DU-145: 59.6), Breast Cancer (MCF7: 77.5, MDA-MB-231/
3
ATCC: 52.6, HS 578 T: 18.5, BT-549: 47.0, T-47D: 47.6, MDA-MB-468: 35.3).
NSC Lung Cancer (A549/ATCC: 13.7, HOP-62: 10.2, NCI-H226: 13.6, NCI-H522: 25.0), Colon Cancer (HT29: 11.3), CNS Cancer (SNB-75: 10.9),
Melanoma (UACC-257: 29.4), Renal Cancer (UO-31: 12.7), Breast Cancer (MDA-MB-468: 18.1).
1
7
8
9/59
1
14/59
Leukaemia (HL-60(TB): 30.6, K-562: 17.7, MOLT-4: 31.7, SR: 24.5), NSC Lung Cancer (A549/ATCC: 20.1, NCI-H522: 17.2), Colon Cancer (HCT-
1
16: 12.7), Melanoma (MALME-3M: 12.2 , UACC-257: 21.8, UACC-62: 11.2), Ovarian Cancer (IGROV1: 15.0), Renal Cancer (A498: 16.0,
CAKI-1: 10.1), Prostate Cancer (PC-3: 10.3).
1
9
0
13/59
59/59
Leukaemia (HL-60(TB): 67.3, K-562: 27.2, MOLT-4: 30.9, SR: 18.5), NSC Lung Cancer (A549/ATCC: 29.3, HOP-62: 12.1, NCI-H522: 37.7), Colon
Cancer (HT29: 17.5), CNS Cancer (U251: 13.0), Melanoma (SK-MEL-2: 13.9, UACC-257: 48.4), Ovarian Cancer (OVCAR-8: 19.6), Renal
Cancer (UO-31: 12.8).
Leukaemia (CCRF-CEM: 93.1, HL-60(TB): 100, K-562: 87.6, MOLT-4: 97.3, PRMI-8226: 79.0, SR: 91.0), NSC Lung Cancer (A549/ATCC: 87.5,
EKVX: 84.5, HOP-62: 87.1, NCI-H226: 77.4, NCI-H23: 67.2, NCI-H322M: 75.0, NCI-H460: 96.7, NCI-H522: 90.1), Colon Cancer (COLO 205:
2
9
5
2
1.4, HCC-2998: 60.4, HCT-116: 81.6, HCT-15: 71.5, HT29: 78.2, KM12: 74.1, SW-620: 67.0), CNS Cancer (SF-268: 78.2, SF-295: 78.6, SF-
39: 96.0, SNB-19: 68.0, SNB-75: 44.8, U251: 79.4), Melanoma (LOX IMVI: 90.3, MALME-3M: 86.0 , M14: 96.6, MDA-MB-435: 62.8, SK-MEL-
: 80.5, SK-MEL-28: 72.88, SK-MEL-5: 100, UACC-257: 100, UACC-62: >100), Ovarian Cancer (IGROV1: 78.8, OVCAR-3: 66.6, OVCAR-4: 65.3,
OVCAR-5: 67.5, OVCAR-8: 83.2, NCI/ADR-RES: 82.2, SK-OV-3: 61.0), Renal Cancer (786-0: 84.6, A498: 54.7, ACHN: 82.9, CAKI-1: 79.6, RXF
3
93: 71.5, SN12C: 68.8, TK-10: 69.5, UO-31: 100), Prostate Cancer (PC-3: 50.8, DU-145: 75.5), Breast Cancer (MCF7: 91.2, MDA-MB-231/
ATCC: 56.8, HS 578 T: 32.0, BT-549: 69.3, T-47D: 70.0, MDA-MB-468: 98.8).
Leukaemia (HL-60(TB): 45.9, K-562: 19.1, MOLT-4: 34.1), NSC Lung Cancer (NCI-H522: 15.7), Colon Cancer (HCT-116: 11.0), CNS Cancer (SNB-
21
22
23
24
8/59
9/59
7
5: 14.2), Renal Cancer (CAKI-1: 11.0), Prostate Cancer (PC-3: 11.5).
Leukaemia (CCRF-CEM: 13.0, HL-60(TB): 43.0, K-562: 14.5, MOLT-4: 29.9), NSC Lung Cancer (A549/ATCC: 32.3, NCI-H522: 14.0), Colon Cancer
HT29: 11.0), Melanoma (SK-MEL-2: 10.9, UACC-257: 40.9).
Leukaemia (HL-60(TB): 44.2, K-562: 37.6, MOLT-4: 32.6), NSC Lung Cancer (A549/ATCC: 22.8), Colon Cancer (COLO 205: 14.6), CNS Cancer
SNB-75: 11.3), Melanoma (UACC-257: 28.6), Ovarian Cancer (SK-OV-3: 14.2), Renal Cancer (UO-31: 10.2).
(
9/59
(
8/59
Leukaemia (MOLT-4: 21.4), NSC Lung Cancer (A549/ATCC: 17.1, NCI-H522: 39.8), Colon Cancer (HT29: 17.9), Melanoma (K-MEL-2: 11.7,
UACC-257: 21.6), Renal Cancer (UO-31: 10.5), Prostate Cancer (PC-3: 18.6).
Leukaemia (MOLT-4: 18.0, PRMI-8226: 12.6, SR: 14.6), NSC Lung Cancer (EKVX: 15.7, NCI-H226: 10.6, NCI-H23: 17.1), Colon Cancer (HCT-116:
Imatinib
20/54
1
8.6, HCT-15: 11.5, HT29: 47.1), CNS Cancer (SF-295: 15.1, SF-539: 24.5, U251: 10.6), Melanoma (LOX IMVI: 11.6, SK-MEL-5: 22.3), Renal
Cancer (A498: 13.7), Prostate Cancer (PC-3: 10.6, DU-145: 14.4), Breast Cancer (MDA-MB-231/ATCC: 11.2, T-47D: 18.6, MDA-MB-
68: 29.1).
4
a
Growth Inhibition percentages (GI%) lower than 10% are not shown.
PCE: Positive cytotoxic effect (ratio between the number of cell lines with percentage growth inhibition from 10 to 100 and the total number of cell lines).
b