Compound

Substituents

Inhibition Rate %^a

IC₅₀ (μM)^b

HeLa

BGC-823

HeLa

BGC-823

43

X=F, Y=H, R=3^’-Cl

46.9

77.5

17.29

3.63

44

X=F, Y=H, R=4^’-Cl

40.3

63.1

20.39

7.83

45

X=F, Y=H, R=3’-F

37.0

65.3

19.82

9.10

46

X=F, Y=H, R=4’-F

20.4

49.5

43.25

11.10

47

X=F, Y=H, R=3’-Cl, 4’-Cl

40.8

56.9

36.69

8.29

48

X=F, Y=H, R=3’-Cl, 4’-F

46.8

67.5

10.18

8.32

49

X=F, Y=H, R=4’-CH₃

41.7

59.4

18.9

7.08

50

X=F, Y=H, R=4’-OCH₃

36.1

35.1

55.76

21.61

51

X=H, Y=OCH₃, R=3’-Cl

35.3

19.5

66.69

>10

52

X=H, Y=OCH₃, R=4’-Cl

31.5

13.1

>10

>10

53

X=H, Y =OCH₃,R=3’-F

31.9

48.1

75.87

11.67

54

X=H, Y=OCH₃,R=4’-F

18.9

37.5

>10

46.41

55

X=H, Y=OCH₃, R=3’-Cl, 4’-Cl

30.8

48.7

45.87

11.45

56

X=H, Y=OCH₃, R=3’-Cl, 4’-F

37.2

20.2

45.84

>10

57

X=H, Y=OCH₃, R=4’-CH₃

30.5

31.1

99.54

61.52

58

X=H, Y=OCH₃, R=4’-OCH₃

21.9

32.0

>10

74.60

59

X=H, Y=OCH₃, R=4’-CH(CH₃)₂

59.1

78.4

7.15

4.65

60

X=H, Y=OCH₃, R=3’-Cl, 4’-CH₃

32.7

24.5

71.26

>10

61

X=H, Y=OCH₃, R=2’-F, 3’-F,4’-F

32.5

27.6

57.88

>10

62

X=H, Y=OCH₃, R=4’-NO₂

35.8

36.8

13.48

>10

63

X=H, Y=OCH₃, R=4’-OH

32.7

25.6

3.58

>10

64

X=H, Y=OCH₃, R=3’-CN

28.6

16.0

30.61

>10

Gefitinib

42.6

46.0

17.12

19.27