Table 5 Optimisation of 9, 15 and 1 on EGFR and UCH-1 and UCH-2 chordoma cell lines.

From: Optimization of the 4-anilinoquin(az)oline scaffold as epidermal growth factor receptor (EGFR) inhibitors for chordoma utilizing a toxicology profiling assay platform

Name

R1

R2

R3

R4

R5

U-CH1

U-CH2

EGFRb

IC50 (μM)a

9

I

H

H

H

H

8.7

> 100

0.83

34

I

H

F

H

H

27

> 100

0.76

35

I

H

H

F

H

8.9

> 100

1.9

36

I

H

H

H

F

2.7

> 100

2.7

37

I

H

H

H

Cl

31

5.0

2.0

15

H

I

H

H

H

17

> 100

2.8

38

H

I

F

H

H

15

> 100

5.2

39

H

I

H

F

H

2.4

15

1.7

40

H

I

H

H

F

> 100

> 100

3.6

41

H

I

H

H

Cl

9.1

16

3.7

1

OMe

OMe

H

H

H

0.63

66

0.019

42

OMe

OMe

F

H

H

6.7

20

0.29

43

OMe

OMe

H

F

H

2.0

7.1

0.060

44

OMe

OMe

H

H

F

> 100

22

0.030

45

OMe

OMe

H

H

Cl

> 100

35

0.018

  1. aCell viability assay (n = 4).
  2. bProQinase in-cell EGFR assay (n = 1).
Back to article page