Table 1.
Cell type | Cell line | GI (%) (10–5 M)a |
||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|
Compound | 11a | 11b | 11d | 11e | 11f | 11i | 11j | 11k | 14a | 15a | 15j | |
Leukaemia | CCRF-CEM | 83 | 65 | 24 | 10 | 20 | 0 | 0 | 0 | 0 | 100b,p | 100b,i′ |
K-562 | 89 | 86 | 23 | 1 | 11 | 0 | 0 | 0 | 2 | 100b,q | 100b,j′ | |
SR | 76 | 84 | 32 | 30 | 30 | 0 | 0 | 14 | 5 | 100b,r | 100b,k′ | |
HL-60(TB) | 100b,c | 100b,l | 30 | 35 | 28 | 0 | 0 | 0 | 2 | 67 | 75 | |
MOLT-4 | 76 | 69 | 34 | 0 | 0 | 0 | 0 | 0 | 3 | 100b,s | 89 | |
RPMI-8226 | 77 | 72 | 10 | 43 | 13 | 0 | 0 | 27 | 15 | 100b,t | 77 | |
Non-small cell lung cancer | A549/ATCC | 74 | 64 | 11 | 20 | 11 | 0 | 14 | 53 | 0 | 68 | 68 |
HOP-62 | 72 | 70 | 10 | 10 | 11 | 13 | 4 | 47 | 4 | 5 | 12 | |
NCI-H460 | 86 | 85 | 0 | 3 | 0 | 0 | 12 | 82 | 0 | 100b,u | 96 | |
NCI-H522 | 74 | 59 | 25 | 21 | 19 | 34 | 7 | 100b,o | 13 | 100b,v | 29 | |
Colon cancer | COLO205 | 100b,d | 86 | 0 | 0 | 0 | 0 | 0 | 35 | 0 | 56 | 57 |
HCT-116 | 81 | 88 | 19 | 24 | 3 | 11 | 0 | 0 | 3 | 100b,w | 95 | |
HCT-15 | 71 | 74 | 17 | 1 | 0 | 0 | 0 | 17 | 3 | 17 | 25 | |
HT-29 | 99 | 90 | 23 | 8 | 12 | 0 | 0 | 23 | 0 | 100b,x | 100b,l′ | |
SW-620 | 70 | 78 | 7 | 0 | 0 | 0 | 0 | 41 | 4 | 100b,z | 100b,m′ | |
KM12 | 75 | 76 | 2 | 0 | 2 | 0 | 0 | 23 | 0 | 55 | 36 | |
CNS cancer | SF-295 | 79 | 73 | 3 | 0 | 0 | 9 | 0 | 31 | 0 | 6 | 0 |
SF-539 | 100b,e | 55 | 3 | 6 | 0 | 12 | 11 | 70 | 0 | 70 | 10 | |
SNB-75 | 67 | 79 | 2 | 11 | 9 | 17 | 15 | 76 | 38 | 24 | 7 | |
U251 | 78 | 61 | 10 | 7 | 5 | 26 | 14 | 78 | 0 | 100b,a′ | 87 | |
SF-268 | 44 | 53 | 11 | 4 | 0 | 3 | 7 | 75 | 11 | 100b,b′ | 21 | |
Melanoma | LOX IMVI | 53 | 61 | 8 | 1 | 3 | 0 | 0 | 15 | 6 | 100b,c′ | 87 |
M14 | 100b,f | 96 | 0 | 0 | 0 | 5 | 0 | 0 | 0 | 45 | 43 | |
MDA-MB-435 | 100b,g | 100b,m | 0 | 0 | 0 | 0 | 0 | 29 | 11 | 31 | 24 | |
UACC-62 | 50 | 69 | 11 | 1 | 2 | 8 | 1 | 16 | 6 | 13 | 0 | |
SK-MEL-5 | 62 | 73 | 7 | 17 | 3 | 0 | 7 | 63 | 4 | 18 | 2 | |
Ovarian cancer | OVCAR-3 | 100b,h | 100b,n | 0 | 0 | 0 | 0 | 0 | 21 | 0 | 18 | 63 |
NCI/ADR-RES | 89 | 88 | 8 | 1 | 0 | 0 | 0 | 34 | 5 | 6 | 11 | |
SK-OV-3 | 78 | 64 | 18 | 13 | 19 | 6 | 0 | 94 | 0 | 0 | 9 | |
OVCAR-8 | 67 | 58 | 12 | 9 | 6 | 0 | 9 | 63 | 8 | 93 | 23 | |
OVCAR-4 | 32 | 28 | 8 | 4 | 0 | – | – | – | 0 | 100b,d′ | 70 | |
Renal cancer | A498 | 100b,i | 71 | 2 | 14 | 0 | 0 | 6 | 58 | 0 | 20 | 26 |
RXF393 | 100b,j | 50 | 3 | 5 | 0 | 9 | 6 | 36 | 0 | 34 | 27 | |
ACHN | 41 | 51 | 0 | 0 | 0 | 19 | 10 | 70 | 8 | 9 | 4 | |
786-0 | 65 | 64 | 0 | 10 | 0 | 9 | 0 | 0 | – | 100b,e′ | 91 | |
TK10 | 51 | 44 | 0 | 10 | 0 | 0 | 0 | 45 | 0 | 87 | 0 | |
Breast cancer | MCF7 | 76 | 78 | 15 | 0 | 0 | 5 | 10 | 17 | 6 | 100b,f′ | 99 |
MDA-MB-468 | 100b,k | 70 | 3 | 30 | 9 | 10 | 6 | 25 | 0 | 57 | 29 | |
T-47D | 53 | 51 | 16 | 16 | 0 | 9 | 20 | 77 | 0 | 50 | 17 | |
MDA-MB-231/ATCC | 62 | 44 | 18 | 30 | 11 | 10 | 6 | 42 | 12 | 100b,g′ | 29 | |
BT-549 | 60 | 64 | 0 | 9 | 0 | 13 | 0 | 4 | 0 | 100b,h′ | 18 | |
Prostate cancer | PC-3 | 88 | 60 | 17 | 15 | 12 | 2 | 9 | 13 | 2 | 46 | 49 |
DU-145 | 75 | 46 | 0 | 0 | 0 | 0 | 0 | 35 | 0 | 55 | 70 |
aData obtained from NCI’s in vitro 60 cell one dose screening at 10−5 M concentration; compounds 11l and 14d were also tested, but no GI was exhibited on the tested cell lines (results are not shown).
bCytotoxic effect; cell growth percent: c-25; d-32; e-7; f -22; g-42; h-6; i-1; j-0.4; k-7; l-14; m-5; n-5; o-4; p-15; q-45; r-16; s-9; t-22; u-10; v-21; w-61; x-10; z-65; a′-74, b′-14, c′-44; d′-33; e′-82; f′-29; g′-23; h′-6; i′-3; j′-53; k′-27; l′-10; m′-30.
The best values in terms of growth inhibition are highlighted in bold.