| ||||||
---|---|---|---|---|---|---|
Compound | R | % inhibition of VEGFR-2 at 80 nM | IC50 (μM)/selective index (SI) | |||
HCT116 | NCI-H460 | 786-O | Detroit 551 | |||
Sunitinib | – | 45 | 4.60 ± 0.23 | 7.51 ± 0.78 | 7.89 ± 0.60 | 9.48 ± 0.18 |
1.32 | 0.81 | 0.76 | ||||
4 | –SO2NH2 | 0 | >10 | >10 | >10 | >10 |
nd | nd | nd | ||||
5 | –SO2NMe2 | 20 | 8.98 ± 0.92 | >10 | >10 | >10 |
>1.11 | nd | nd | ||||
6 | –SO2NEt2 | 0 | 4.20 ± 0.57 | >10 | >10 | >10 |
>2.38 | nd | nd | ||||
7 | –SO2N(CH2CH2Cl)2 | 46 | 3.65 ± 0.19 | >10 | >10 | 6.06 ± 0.40 |
1.66 | <0.61 | <0.61 | ||||
8 | –SO2NHPh | 15 | >10 | >10 | >10 | >10 |
nd | nd | nd | ||||
9 | –SO2NH(4-CF3-Ph) | 0 | >10 | >10 | >10 | >10 |
nd | nd | nd | ||||
10 | –NHMs | 4 | >10 | >10 | >10 | >10 |
nd | nd | nd | ||||
11 | –CF3 | 0 | >10 | 7.22 ± 1.01 | 8.49 ± 0.46 | >10 |
nd | >1.39 | >1.18 | ||||
12 | –NO2 | 13 | >10 | 6.61 ± 0.80 | >10 | >10 |
nd | >1.51 | nd | ||||
13 | –OMe | 41 | 3.06 ± 0.67 | 6.37 ± 1.09 | 7.86 ± 0.30 | >10 |
>3.27 | >1.57 | >1.27 | ||||
14 | –OH | 58 | 2.83 ± 0.40 | >10 | >10 | >10 |
3.53 | nd | nd | ||||
15 | –SH | 57 | 2.34 ± 0.20 | >10 | >10 | >10 |
>4.27 | nd | nd |