Table 1.
Cytotoxic activity expressed by IC50 μM (95% CI) of compounds 4-7, 9-10, 13-16, 19-22, 25, 26, 28, 29, 36-38, 39, 40, 48 and 49 in cancer and normal cell lines after 72 h exposure, obtained by nonlinear regression for all cell lines from three independent experiments.
| Compd | HL-60 | HCT-116 | PC3 | SF295 | MDA-MB-435 | OVCAR-8 | PBMC | V79 | L929 |
|---|---|---|---|---|---|---|---|---|---|
| 4 | >13.99 | >13.99 | >13.99 | >13.99 | >13.99 | >13.99 | >13.99 | >13.99 | >13.99 |
| 5 | 1.66 (1.09-2.22) |
2.96 (2.19-3.81) |
2.15 (1.94-2.36) |
2.05 (1.52-2.54) |
2.72 (2.33-3.28) |
1.48 (1.38-1.62) |
6.11 (5.65-6.88) |
3.67 (2.89-4.45) |
4.13 (3.28-4.87) |
| 6 | 2.00 (1.74-2.25) |
4.90 (4.62-5.76) |
2.60 (2.18-2.86) |
1.88 (1.47-2.26) |
1.49 (1.30-1.70) |
3.09 (1.98-4.85) |
4.16 (3.93-4.44) |
3.65 (3.21-3.81) |
3.30 (2.81-3.58) |
| 7 | 5.46 4.87-6.10) |
2.24 (1.71-2.53) |
3.89 (3.18-4.47) |
4.20 (3.93-4.89) |
3.85 (3.49-4.33) |
2.55 (2.05-2.95) |
4.45 (3.91-5.14) |
5.20 (4.62-5.43) |
5.46 (4.97-6.00) |
| 9 | 1.43 (1.32-1.54)a |
2.48 (2.32-2.68) |
1.68 (1.52-2.02) |
1.93 (1.76-2.12)a |
1.54 (1.46-1.62)a |
2.24 (1.99-2.70) |
3.58 (3.34-3.86)a |
2.40 (2.29-2.51) |
2.04 (1.74-2.43) |
| 10 | 1.22 (1.13-1.35) |
1.11 (0.84-1.26) |
1.90 (1.60-2.01) |
1.52 (1.44-1.67) |
1.31 (1.22-1.52) |
0.92 (0.88-1.22) |
1.87 (1.45-2.26) |
2.17 (2.03-2.31) |
1.74 (1.67-1.94) |
| 13 | 2.59 (2.30-2.94) |
4.60 (3.78-5.59) |
5.15 (4.63-5.80) |
>14.56 | 3.93 (3.44-4.40) |
7.13 (6.12-8.30) |
6.46 (5.50-7.10) |
6.06 (5.36-6.55) |
5.33 (5.15-5.53) |
| 14 | 2.23 (1.78-2.67) |
3.30 (2.90-3.68) |
4.09 (3.49-4.57) |
3.04 (2.64-3.82) |
2.52 (2.23-2.75) |
3.53 (3.34-3.75) |
3.16 (2.86-3.49) |
4.20 (3.82-4.90) |
3.68 (3.45-4.34) |
| 15 | 1.08 (0.86-1.49) |
1.28 (1.04-1.57) |
1.71 (1.44-2.03) |
1.08 (0.94-1.46) |
0.88 (0.76-1.06) |
0.68 (0.43-1.06) |
3.33 (2.94-3.56) |
3.78 (3.73-3.94) |
3.38 (3.06-3.65) |
| 16 | 1.59 (1.34-1.87) |
2.54 (1.55-2.88) |
2.95 (2.22-3.47) |
2.65 (2.39-3.34) |
2.15 (2.00-2.32) |
2.80 (2.45-3.34) |
3.23 (2.43-3.96) |
4.03 (3.29-4.63) |
3.77 (3.06-4.48) |
| 19 | 0.26 (0.20-0.35) |
1.48 (1.34-1.69) |
1.86 (1.69-2.39) |
2.59 (2.36-2.85) |
2.04 (1.78-2.18) |
2.53 (2.33-2.74) |
2.80 (2.30-3.35) |
2.16 (1.83-2.68) |
2.50 (2.33-2.77) |
| 20 | 3.08 1.48-6.46b |
0.89 (0.82-1.00) |
1.74 (1.22-2.15) |
3.23 2.38-4.38b |
1.19 1.08-1.34b |
1.34 (1.15-1.45) |
nd | 3.27 (2.97-3.53) |
2.67 (2.26-3.49) |
| 21 | 0.07 (0.02-0.16) |
0.14 (0.11-0.25) |
0.38 (0.29-0.67) |
0.34 (0.20-0.45) |
0.23 (0.16-0.38) |
0.20 (0.14-0.43) |
1.39 (1.12-1.53) |
1.13 (1.03-1.26) |
0.94 (0.86-1.15) |
| 22 | 1.29 (1.03-1.59) |
2.52 (2.00-2.88) |
2.43 (1.87-3.21) |
1.31 (1.10-1.59) |
1.06 (0.99-1.12) |
2.26 (1.66-3.06) |
1.76 (1.44-2.11) |
2.65 (1.76-3.16) |
2.30 (1.89-2.71) |
| 25 | 0.82 (0.55-1.45) |
0.63 (0.43-0.86) |
0.51 (0.24-0.59) |
0.39 (0.31-0.43) |
0.39 (0.27-0.59) |
0.35 (0.12-0.47) |
1.80 (1.57-2.15) |
0.82 (0.67-1.14) |
1.06 (0.94-1.18) |
| 26 | 0.13 (0.04-0.29) |
0.24 (0.18-0.31) |
0.24 (0.20-0.27) |
0.22 (0.20-0.24) |
0.29 (0.22-0.33) |
0.07 (0.02-0.13) |
1.31 (1.11-1.40) |
0.44 (0.22-0.60) |
0.62 (0.49-0.78) |
| 28 | 0.31 (0.20-0.43) |
0.24 (0.16-0.39) |
0.39 (0.16-0.63) |
0.35 (0.12-0.47) |
0.20 (0.04-0.27) |
0.35 (0.27-0.43) |
3.21 (2.58-4.27) |
2.47 (2.27-3.02) |
2.15 (1.88-2.70) |
| 29 | 0.82 (0.58-1.09) |
2.42 (1.80-3.26) |
1.40 (1.13-1.71) |
0.98 (0.69-1.44) |
0.62 (0.42-1.02) |
0.91 (0.75-1.11) |
2.80 (2.53-3.04) |
2.02 (1.64-2.44) |
2.15 (2.04-2.53) |
| 36 | 2.14 (1.99-2.49) |
3.25 (3.01-3.76) |
2.25 (1.92-2.40) |
2.93 (2.77-3.08) |
2.01 (1.64-2.47) |
2.58 (2.21-2.97) |
6.34 (5.70-6.66) |
2.51 (2.03-2.86) |
3.43 (3.01-3.78) |
| 37 | 1.11 (0.96-1.23) |
1.67 (1.43-2.05) |
2.29 (2.07-2.53) |
1.61 (1.43-1.89) |
1.43 (1.17-1.81) |
2.37 (1.87-2.49) |
3.86 (3.78-4.04) |
3.03 (2.87-3.40) |
3.30 (2.97-3.62) |
| 38 | 1.13 (0.78-1.20) |
1.72 (1.42-1.98) |
2.08 (1.84-2.41) |
0.97 (0.85-1.28) |
3.09 (2.72-3.76) |
1.89 (1.46-2.67) |
4.75 (4.44-5.06) |
3.99 (3.40-4.49) |
3.83 (3.76-3.97) |
| 39 | 2.21 (1.91-2.56) |
4.27 (4.22-4.52) |
2.16 (1.76-2.71) |
3.41 (3.11-3.62) |
2.36 (1.91-2.91) |
3.51 (3.16-4.27) |
8.64 (7.53-9.69) |
5.77 (4.62-6.73) |
5.17 (4.27-5.97) |
| 40 | >12.68 | >12.68 | >12.68 | >12.68 | >12.68 | >12.68 | >12.68 | >12.68 | >12.68 |
| 48 | 8.26 (8.00-9.17) |
7.22 (6.78-7.56) |
7.79 (7.46-8.07) |
5.58 (5.41-6.00) |
6.82 (6.23-7.16) |
7.90 (7.37-8.19) |
7.45 (7.24-7.71) |
6.74 (6.04-7.05) |
7.16 (6.91-7.50) |
| 49 | >8.67 | >8.67 | >8.67 | >8.67 | >8.67 | >8.67 | >8.67 | >8.67 | >8.67 |
| β-lap. | 1.57 1.11-1.69 |
0.87 0.74-0.95 |
1.65 1.40-1.94 |
0.95 0.70-1.03 |
0.25 0.16-0.33 |
1.16 0.97-1.25 |
>20.63 | - | - |
| DOXO | 0.06 0.02-0.09 |
0.15 0.09-0.21 |
0.02 0.02-0.04 |
0.51 0.43-0.58 |
0.96 0.87-1.10 |
0.41 0.36-0.49 |
0.55 0.41-0.58 |
0.28 0.21-0.36 |
0.23 0.15-0.30 |