Code

numbers^a,b

R or R₁

X

IC₅₀

(MCF7, nM)

Competition assay^c

9

R = 2-Me

O

30

++

10

R = 3-Me

O

57

+++

11

R = 4-Me

O

150

−

12

R = 4-OMe

O

160

+

13

R = 4-NMe₂

O

500

N/A

14

R = 4-OH

O

>1000

N/A

15

R = H

O

>1000

N/A

17

R = 2-Prop

O

69

+

18

R = 2-OMe

O

220

N/A

19

R = 2-OEt

O

83

+++

21

R = 2-F

O

61

++

24

R = 2-Me, 3-Me

O

50

+++

25

R = 2-Me, 4-Me

O

50

+

26

R = 2-Me, 5-Me

O

14

+++

27

R = 2-Me, 4-Me, 5-Me

O

66

++

28

R = 2-Cl, 4-Cl, 5-Cl

O

30

+++

29

R = 2-Cl, 4-Cl, 6-Cl

O

170

N/A

30

R = 2-F, 4-F

O

55

++

31

R = 2-F, 6-F

O

32

+++

32

R = 2-F, 3-F, 4-F, 5-F, 6-F

O

320

N/A

34

R = 3-OMe

O

34

+++

37

R = 3-F

O

54

++

38

R = 3-I

O

18

+++

39

R = 3-NO₂

O

60

+++

40

R = 3-NH₂

O

270

N/A

41

R = 3-Me, 5-Me

O

47

+++

42

R = 3-Me, 4-Me, 5-Me

O

49

+++

43

R = 3-OMe, 4-OMe

O

88

+++

44

R = 3-OMe, 5-OMe

O

10

+++

45

R = 3-OMe, 4-OMe, 5-OMe

O

5.0

+++

46

R = 3-Cl, 5-Cl

O

18

+++

47

R = 3-F, 4-F

O

100

+