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Table 1 Enzymatic and cellular inhibition activities of 4–15 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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BMC Chemistry

ISSN: 2661-801X

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