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Table 1 Enzymatic and cellular inhibition activities of 415 and sunitinib

From: Structural optimization and evaluation of novel 2-pyrrolidone-fused (2-oxoindolin-3-ylidene)methylpyrrole derivatives as potential VEGFR-2/PDGFRβ inhibitors

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
  1. nd not detected
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