The in vitro antiproliferation activities of combretastatin A-4 sulfamate and sulfamide derivatives against on six human tumor cellsa.
| |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Compounds | IC50 (mean ± SD, μM)a | ||||||||
| Entry | R | R1(R2)N | X | HTC-116 | HeLa | HepG2 | MGC803 | MKN45 | MCF-7 |
| CA-4 | — | — | — | 0.0047 ± 0.0008 | 0.0029 ± 0.0001 | 0.0029 ± 0.0007 | 0.0060 ± 0.0006 | 0.0081 ± 0.0004 | 0.14 ± 0.02 |
| EMATE | — | — | — | 0.90 ± 0.04 | 0.63 ± 0.06 | 0.85 ± 0.05 | 0.48 ± 0.09 | 0.54 ± 0.12 | 0.07 ± 0.10 |
| 16a (Z) | OMe | NH2 | O | 0.0050 ± 0.0005 | 0.0061 ± 0.0003 | 0.0036 ± 0.0002 | 0.0047 ± 0.0006 | 0.0095 ± 0.0004 | 0.11 ± 0.04 |
| 16b (E) | OMe | NH2 | O | 1.57 ± 0.07 | 4.50 ± 0.07 | 0.87 ± 0.09 | 2.98 ± 0.07 | 10.52 ± 0.04 | 5.44 ± 0.05 |
| 16c (Z) | OCF2H | NH2 | O | 9.11 ± 0.04 | 7.82 ± 0.05 | 4.81 ± 0.06 | 9.00 ± 0.05 | 12.52 ± 0.04 | 0.29 ± 0.05 |
| 16d (E) | OCF2H | NH2 | O | 12.84 ± 0.03 | 8.42 ± 0.04 | 5.54 ± 0.05 | 9.24 ± 0.04 | 13.84 ± 0.04 | 13.79 ± 0.03 |
| 16e (Z) | OEt | NH2 | O | 0.55 ± 0.07 | 0.48 ± 0.08 | 0.41 ± 0.05 | 0.27 ± 0.07 | 0.32 ± 0.07 | 0.30 ± 0.06 |
| 16f (E) | OEt | NH2 | O | 9.12 ± 0.04 | 5.64 ± 0.05 | 2.63 ± 0.07 | 7.63 ± 0.05 | 8.05 ± 0.05 | 13.71 ± 0.03 |
| 16g (Z) | H | NH2 | O | 9.50 ± 0.03 | 16.30 ± 0.03 | 9.36 ± 0.05 | 8.53 ± 0.04 | 15.32 ± 0.02 | 11.10 ± 0.04 |
| 16h (E) | H | NH2 | O | 40.30 ± 0.04 | 19.00 ± 0.03 | 11.85 ± 0.03 | 27.03 ± 0.02 | 25.04 ± 0.02 | 27.44 ± 0.02 |
| 16i (Z) | OMe | NHMe | O | 0.0113 ± 0.0003 | 0.0034 ± 0.0005 | 0.0039 ± 0.0010 | 0.0037 ± 0.0006 | 0.0073 ± 0.0003 | 0.53 ± 0.03 |
| 16j (Z) | OMe | N(Me)2 | O | 0.37 ± 0.07 | 14.26 ± 0.04 | 9.96 ± 0.03 | 7.14 ± 0.03 | 8.95 ± 0.37 | 11.06 ± 0.04 |
| 19a (Z) | OMe | NH2 | NH | 3.29 ± 0.77 | 0.27 ± 0.06 | 0.75 ± 0.06 | 0.50 ± 0.07 | 9.56 ± 0.09 | 11.19 ± 0.06 |
| 19b (E) | OMe | NH2 | NH | 8.65 ± 0.04 | 0.38 ± 0.05 | 7.53 ± 0.06 | 6.19 ± 0.06 | 18.87 ± 0.03 | 17.09 ± 0.04 |
| 17a b | OMe | NH2 | O | 2.63 ± 0.08 | 9.04 ± 0.04 | 1.06 ± 0.05 | 3.61 ± 0.08 | 11.87 ± 0.04 | 5.91 ± 0.06 |
| 17a b | OCF2H | NH2 | O | 26.48 ± 0.02 | 35.65 ± 0.01 | 15.88 ± 0.02 | 23.26 ± 0.02 | 71.38 ± 0.02 | 52.74 ± 0.03 |
| 17c b | OEt | NH2 | O | 10.16 ± 0.03 | 2.930 ± 0.07 | 3.65 ± 0.07 | 3.59 ± 0.06 | 7.67 ± 0.06 | 14.75 ± 0.02 |
| 17d b | H | NH2 | O | 52.49 ± 0.02 | 27.06 ± 0.03 | 12.03 ± 0.03 | 17.64 ± 0.04 | 25.70 ± 0.03 | >100 |
| 20 b | OMe | NH2 | NH | 30.63 ± 0.04 | 2.926 ± 0.07 | 8.10 ± 0.05 | 8.21 ± 0.04 | 73.88 ± 0.05 | 20.13 ± 0.03 |
a
The experiment was carried out using an EnoGeneCellTM counting Kit-8 (CCK-8) assay.
b
Saturated bond linked compound.