Table 1 In vitro growth inhibition% (GI%) of NCI 60 cancer cell line panel after treatment with 10 μM of the oxindole–benzothiazoles 9a–c and 9e-r
Cell name | GI% | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
9a | 9b | 9c | 9e | 9f | 9g | 9h | 9i | 9j | 9k | 9l | 9m | 9n | 9o | 9p | 9q | 9r | Milciclib | |
Leukemia | ||||||||||||||||||
CCRF-CEM | 20.22 | 23.64 | 60.17 | –a | 21.91 | 41.07 | 47.56 | 44.24 | 34.81 | 24.47 | 15.16 | 40.05 | 16.11 | 57.64 | 9.28 | 81.35 | 42.87 | 89.60 |
HL-60(TB) | – | 8.38 | 15.59 | – | 29.39 | 15.30 | – | – | – | 6.09 | – | – | – | 7.99 | – | – | – | 127.0 |
K-562 | – | 20.57 | 30.54 | – | 22.52 | 32.23 | 26.17 | 21.95 | – | 29.20 | 18.70 | 11.23 | 6.70 | 64.36 | – | 50.00 | 24.52 | 94.6 |
MOLT-4 | 8.23 | 29.12 | 47.19 | – | 36.74 | 49.06 | 43.65 | 45.30 | 9.01 | 43.70 | 36.40 | 23.70 | 13.07 | 36.32 | – | 71.36 | 13.12 | 97.70 |
RPMI-8226 | 21.80 | 30.53 | 48.87 | – | 29.01 | 50.80 | 54.14 | 47.68 | 22.11 | 29.96 | 25.41 | 25.46 | 14.26 | 66.93 | – | 46.48 | 19.17 | 99.60 |
SR | – | 18.71 | 20.98 | 6.46 | 43.03 | 18.95 | – | – | – | 17.83 | 16.68 | 12.20 | ndb | 35.47 | – | 18.57 | – | 101.8 |
Non-small cell lung cancer | ||||||||||||||||||
A549/ATCC | 11.63 | 28.01 | 25.86 | – | 29.34 | 16.44 | 24.44 | 18.26 | 5.97 | 26.29 | 17.13 | – | – | 39.87 | 7.06 | 20.18 | 7.78 | 108 |
EKVX | 37.48 | 24.46 | 25.93 | 53.99 | 19.72 | 29.56 | 27.92 | 24.10 | 26.64 | 66.74 | 66.66 | – | – | 55.62 | 9.22 | 25.37 | 7.18 | 94.3 |
HOP-62 | – | 51.18 | – | – | 74.09 | – | – | – | – | 6.81 | 13.44 | nd | – | nd | nd | nd | nd | 109.50 |
HOP-92 | 6.37 | 35.86 | – | nd | 51.76 | 34.60 | 23.13 | 31.66 | 30.70 | nd | nd | – | – | 15.22 | 99.07 | 52.70 | 32.33 | 96.20 |
NCI-H226 | 23.61 | 105.34 | 23.90 | 11.52 | 106.99 | 45.16 | 26.01 | 29.04 | 21.82 | 18.20 | 12.06 | – | – | 5.08 | 67.22 | 24.77 | 10.50 | 87.70 |
NCI-H23 | 6.36 | 85.13 | 17.94 | 7.05 | 40.56 | 25.24 | 13.40 | 11.65 | 22.82 | 17.71 | 17.03 | 14.06 | 12.32 | 84.74 | 47.90 | 42.70 | 20.81 | 97.60 |
NCI-H322M | – | 19.44 | – | – | 17.70 | 10.24 | 6.24 | 5.89 | 6.18 | – | – | – | 10.32 | 9.70 | 6.14 | – | – | 84.90 |
NCI-H460 | – | 34.24 | 6.01 | – | 18.32 | – | – | – | – | 8.94 | 5.26 | 17.38 | – | 106.89 | – | 44.39 | – | 92.50 |
NCI-H522 | – | 37.21 | – | 11.15 | 51.70 | 33.32 | – | 7.04 | – | 28.39 | 25.73 | 7.23 | – | 5.70 | 42.45 | 21.77 | 8.27 | 129.40 |
Colon cancer | ||||||||||||||||||
COLO 205 | – | – | – | – | – | 25.08 | 7.03 | – | – | – | – | nd | – | nd | nd | nd | nd | 180.1 |
HCC-2998 | – | 19.53 | – | – | 11.62 | – | – | – | – | – | – | – | – | 44.35 | – | – | – | 89.6 |
HCT-116 | – | 53.56 | 18.17 | – | 53.40 | 20.48 | 22.91 | 17.55 | 7.08 | 13.42 | 7.62 | 41.54 | – | 87.90 | 47.25 | 72.84 | 30.23 | 99.8 |
HCT-15 | 8.99 | 31.29 | 40.05 | – | 17.46 | 25.54 | 5.56 | 9.87 | 5.47 | 31.91 | 21.00 | 10.77 | 9.62 | 127.40 | – | 36.40 | – | 96.9 |
HT29 | nd | nd | nd | – | – | nd | nd | nd | nd | 14.83 | 9.08 | – | – | 20.32 | – | 6.74 | – | 116.2 |
KM12 | 6.23 | 18.69 | 15.67 | – | 15.34 | 8.64 | 8.90 | 8.46 | 5.79 | 22.47 | 12.55 | – | – | 36.53 | – | 17.57 | – | 99.4 |
SW-620 | – | – | – | – | – | – | – | – | – | – | – | 29.93 | 6.33 | 148.26 | – | 51.82 | 7.61 | 88.5 |
CNS cancer | ||||||||||||||||||
SF-268 | 6.56 | 43.82 | 13.85 | – | 45.84 | 5.11 | – | – | – | – | 8.60 | – | 5.27 | 51.91 | 53.94 | 27.89 | – | 92.00 |
SF-295 | 14.46 | 44.34 | 20.67 | – | 32.61 | 29.36 | 19.06 | 13.86 | 11.71 | 38.31 | 33.14 | – | – | 31.59 | 89.39 | 23.77 | – | 84.70 |
SF-539 | 5.56 | 76.88 | 5.44 | – | 110.59 | 9.46 | 9.04 | 6.47 | – | 30.36 | 9.75 | 10.76 | 11.49 | 12.44 | 65.68 | 34.10 | 21.62 | 128.60 |
SNB-19 | 6.15 | 74.25 | 7.69 | – | 81.08 | 13.10 | 8.33 | 11.58 | 5.77 | – | – | – | – | 49.50 | 86.59 | 63.00 | 48.19 | 87.7 |
SNB-75 | – | 54.28 | – | – | 84.86 | – | – | – | – | – | 10.42 | – | – | – | 120.44 | 15.62 | – | 120.6 |
U251 | – | 56.51 | – | – | 86.92 | 8.36 | 5.89 | – | – | – | – | 13.36 | – | 143.46 | 78.07 | 63.50 | 30.21 | 91.50 |
Melanoma | ||||||||||||||||||
LOX IMVI | – | 84.01 | 9.06 | 8.86 | 59.05 | 25.54 | – | – | – | 13.16 | 19.74 | 18.28 | – | 160.95 | 13.12 | 72.29 | 38.27 | 94.70 |
MALME-3M | – | 57.82 | 13.58 | – | 55.98 | 13.82 | 16.42 | 12.81 | 12.74 | 2.32 | 6.30 | – | 18.46 | 35.23 | 8.36 | 26.21 | 11.71 | 108.70 |
M14 | – | 11.64 | 5.86 | – | 8.00 | – | 9.67 | 7.92 | 8.57 | – | – | – | – | 39.13 | – | 23.59 | 9.47 | 87.5 |
MDA-MB-435 | – | 17.86 | 19.69 | – | 14.63 | 10.97 | – | – | 6.00 | – | 5.27 | – | – | 96.57 | – | 37.37 | – | 78.9 |
SK-MEL-2 | nd | nd | nd | – | nd | nd | nd | nd | nd | 12.78 | 9.60 | – | – | 26.06 | 115.65 | 56.54 | 17.63 | nd |
SK-MEL-28 | – | – | – | – | – | – | – | – | – | – | – | – | 6.91 | 37.85 | – | – | – | 83.80 |
SK-MEL-5 | 13.43 | 62.70 | 44.97 | 5.89 | 43.95 | 95.02 | 62.94 | 51.82 | 24.59 | 23.55 | 19.70 | – | 7.31 | 24.21 | 5.61 | 12.80 | – | 92.70 |
UACC-257 | 6.77 | – | – | – | 13.04 | – | – | – | 5.08 | – | – | – | – | – | – | – | – | 114.80 |
UACC-62 | 13.82 | 33.71 | 28.02 | 10.86 | 25.55 | 46.29 | 34.75 | 25.33 | 11.06 | 32.61 | 35.62 | – | 13.88 | – | 19.19 | 12.95 | – | 109.5 |
Ovarian cancer | ||||||||||||||||||
IGROV1 | – | 35.91 | – | – | 42.62 | 7.95 | 6.64 | – | – | – | 11.35 | – | – | 18.68 | 41.60 | 16.12 | – | 97.50 |
OVCAR-3 | – | 79.13 | – | – | 81.63 | – | – | – | – | – | – | – | – | 94.12 | – | 31.89 | – | 79.30 |
OVCAR-4 | 13.08 | 99.49 | 32.22 | – | 90.58 | 27.14 | 20.46 | 20.14 | 5.61 | 13.16 | 11.40 | 16.50 | - | 68.35 | 13.06 | 25.24 | – | 87.10 |
OVCAR-5 | – | 7.29 | – | – | – | – | – | – | – | 8.99 | – | – | 7.10 | 9.28 | – | – | – | 90.90 |
OVCAR-8 | – | 57.37 | 19.15 | – | 71.28 | 10.62 | 12.04 | 11.59 | – | 12.69 | 10.38 | 20.84 | – | 93.38 | 38.18 | 59.73 | 38.56 | 91.10 |
NCI/ADR-RES | – | 71.87 | 25.58 | 6.89 | 49.76 | 28.45 | 14.65 | 10.58 | 6.51 | 20.56 | 19.73 | 28.96 | 14.31 | 130.36 | 19.93 | 47.55 | 27.04 | 90.10 |
SK-OV-3 | – | 15.84 | – | – | 17.03 | 8.22 | 14.52 | 9.98 | – | – | – | nd | – | nd | nd | nd | nd | 116.90 |
Renal cancer | ||||||||||||||||||
786-0 | – | 57.65 | 5.40 | – | 101.23 | – | 9.21 | 5.62 | – | 22.12 | 16.93 | - | 44.99 | 75.63 | 87.35 | 44.24 | 20.37 | 87.70 |
A498 | – | 5.48 | – | – | 12.61 | – | – | – | – | – | – | – | – | – | 20.06 | – | – | 161.60 |
ACHN | – | 52.92 | 9.04 | 18.45 | 64.71 | 14.78 | 11.83 | 6.51 | 11.44 | 26.60 | 22.74 | 19.82 | 8.57 | 96.99 | 76.97 | 59.32 | 30.78 | 90.4 |
CAKI-1 | 22.46 | 41.90 | 28.09 | 6.21 | 51.85 | 34.75 | 36.68 | 24.98 | 28.19 | 39.78 | 40.19 | 9.28 | 12.63 | 72.22 | 45.22 | 50.03 | 29.61 | 92.30 |
RXF 393 | 5.86 | 134.59 | 23.06 | – | 82.91 | 35.85 | 25.38 | 15.41 | 9.05 | 37.81 | 14.21 | – | nd | 129.01 | 99.84 | 32.76 | 15.08 | 148.20 |
SN12C | 7.64 | 61.93 | 12.43 | 8.28 | 67.11 | 18.49 | 9.88 | 14.66 | 11.67 | 14.00 | 16.14 | 7.15 | 5.76 | 24.01 | 37.68 | 36.67 | 20.61 | 88.70 |
TK-10 | – | 93.55 | – | – | 55.14 | – | – | – | – | – | – | 10.32 | – | 86.88 | 96.63 | 62.99 | 36.32 | 112.5 |
UO-31 | 26.54 | 27.53 | 35.66 | – | 21.89 | 41.81 | 38.34 | 30.29 | 25.41 | 33.24 | 30.14 | – | – | 44.24 | 19.08 | 20.65 | 15.64 | 108.7 |
Prostate cancer | ||||||||||||||||||
PC-3 | 19.26 | 22.82 | 43.83 | nd | 27.83 | 44.41 | 46.62 | 43.62 | 18.80 | nd | nd | 7.63 | – | 49.56 | 11.94 | 26.21 | 16.13 | 92.10 |
DU-145 | 6.07 | 22.75 | 6.75 | – | 14.27 | – | – | – | 6.78 | – | – | 5.42 | 7.08 | 130.12 | – | 19.41 | – | 84.50 |
Breast cancer | ||||||||||||||||||
MCF7 | 25.11 | 64.25 | 18.66 | 15.86 | 55.39 | 26.62 | 37.74 | 23.12 | 25.07 | 35.93 | 35.92 | 33.97 | 25.33 | 82.77 | 17.21 | 57.82 | 35.42 | 89.60 |
MDA-MB-231/ATCC | – | 63.76 | – | 15.59 | 55.33 | 18.32 | 13.89 | 10.30 | 8.73 | 19.83 | 27.34 | 9.78 | 12.37 | 75.41 | 49.20 | 59.98 | 42.55 | 85.30 |
HS 578T | 5.85 | 58.35 | – | – | 75.23 | 16.30 | 9.01 | – | – | 8.19 | – | – | 5.72 | 34.64 | 96.22 | 74.27 | 46.81 | nd |
BT-549 | – | 50.79 | 18.71 | – | 86.84 | 25.83 | 18.44 | 16.10 | – | 7.55 | – | – | – | 33.89 | 54.51 | 23.63 | 21.16 | 94.80 |
T-47D | 12.02 | 48.54 | 36.38 | – | 60.76 | 29.32 | 41.06 | 37.57 | – | 40.62 | 41.03 | nd | 13.50 | nd | nd | nd | nd | 105.70 |
MDA-MB-468 | – | 90.93 | 29.51 | 5.76 | 63.10 | 50.47 | 26.10 | 30.66 | 6.21 | 27.13 | 19.79 | 8.24 | – | 60.54 | 17.86 | – | – | 113.40 |
Mean GI% | – | 44.28 | 12.24 | – | 43.78 | 15.46 | 9.27 | 6.32 | – | 14.92 | 12.52 | 6.03 | – | 55.91 | 30.34 | 31.16 | 10.08 | > 100 |