From: Structural optimization and evaluation of novel 2-pyrrolidone-fused (2-oxoindolin-3-ylidene)methylpyrrole derivatives as potential VEGFR-2/PDGFRβ inhibitors
Compound
R
IC50 (nM)
% inhibition of Aurora A at 1.0 μM
VEGFR-2
PDGFRβ
Sunitinib
–
151.8
94.5
50.7
7
–SO2N(CH2CH2Cl)2
23.7
63.2
94.4
13
–OMe
47.8
76.2
92.9
14
–OH
25.9
28.5
93.6
15
–SH
14.6
12.1
96.4