Table 1 The in vitro antiproliferative effects of the synthesized compounds.

From: Design, synthesis and evaluation of novel tetrahydropyridothienopyrimidin-ureas as cytotoxic and anti-angiogenic agents

Compound

R

X

MCF-7

PC-3

SW480

HEPG-2

HUVEC

11a

H

C

23.34 ± 0.18

34.44 ± 1.64

24.52 ± 0.72

7.34 ± 0.01

19.06 ± 0.12

11b

3-Me

C

8.22 ± 0.09

46.77 ± 1.49

67.65 ± 2.53

48.10 ± 0.22

18.89 ± 0.09

11c

4-Me

C

42.87 ± 0.32

32.21 ± 0.30

70.15 ± 2.71

24.57 ± 0.39

26.12 ± 0.15

11d

4-OMe

C

51.92 ± 0.47

43.96 ± 1.52

45.07 ± 1.70

43.92 ± 0.16

44.15 ± 0.22

11e

3-F

C

13.02 ± 0.18

42.83 ± 1.82

65.60 ± 1.74

9.84 ± 0.06

27.48 ± 0.07

11f

4-F

C

45.04 ± 0.41

41.43 ± 0.46

61.29 ± 2.02

30.69 ± 0.44

47.98 ± 0.27

11g

4-Cl

C

62.38 ± 2.94

41.60 ± 1.10

56.53 ± 1.28

46.96 ± 0.35

27.29 ± 0.19

11h

3,4-DiCl

C

8.52 ± 0.02

70.15 ± 1.92

64.16 ± 2.2

53.71 ± 0.5

7.44 ± 0.06

11i

3-Cl-4-Me

C

50.82 ± 0.54

41.76 ± 1.22

69.58 ± 1.88

3.33 ± 0.07

24.63 ± 0.22

11j

3-CF3

C

68.94 ± 0.63

73.77 ± 2.92

46.79 ± 1.13

62.99 ± 0.64

67.10 ± 1.85

11k

3-CF3-4-Cl

C

24.66 ± 0.24

23.15 ± 0.21

63.47 ± 1.37

28.46 ± 0.25

37.56 ± 0.31

11l

2-Me

N

2.80 ± 0.03

6.11 ± 0.08

14.98 ± 0.38

9.94 ± 0.07

2.53 ± 0.05

11m

3-Me

N

3.35 ± 0.01

11.79 ± 0.11

61.23 ± 0.44

27.76 ± 0.13

1.15 ± 0.03

11n

4-Me

N

2.67 ± 0.21

11.35 ± 0.09

6.84 ± 0.05

7.20 ± 0.03

2.09 ± 0.08

11o

3-OMe

N

14.63 ± 0.07

33.65 ± 1.41

65.80 ± 0.28

69.32 ± 0.52

20.58 ± 0.50

11p

4-OMe

N

3.72 ± 0.55

43.49 ± 1.62

29.40 ± 1.01

67.40 ± 0.33

2.86 ± 0.05

11q

3-F

N

9.17 ± 0.04

4.50 ± 0.03

21.79 ± 0.72

74.26 ± 2.12

10.13 ± 0.05

11r

4-F

N

5.69 ± 0.03

18.98 ± 0.11

66.34 ± 1.24

67.49 ± 1.38

48.24 ± 0.62

11s

2-Cl

N

4.69 ± 0.09

8.94 ± 0.03

30.50 ± 0.12

26.26 ± 0.24

6.87 ± 0.03

11t

3-Cl

N

12.68 ± 0.05

3.02 ± 1.12

14.58 ± 0.32

84.95 ± 3.40

67.00 ± 2.02

11u

4-Cl

N

8.10 ± 0.02

4.96 ± 0.18

60.66 ± 1.13

27.77 ± 1.84

2.08 ± 0.01

11v

3,4-DiCl

N

10.37 ± 0.03

55.30 ± 1.82

67.70 ± 1.55

26.37 ± 0.90

68.37 ± 1.44

11w

3-Cl-4-Me

N

6.80 ± 0.05

9.42 ± 0.63

71.87 ± 1.10

38.45 ± 0.42

6.23 ± 0.03

11x

3-CF3

N

9.36 ± 0.06

32.93 ± 0.61

60.55 ± 0.41

44.61 ± 0.52

9.15 ± 0.02

11y

3-CF3-4-Cl

N

20.48 ± 0.11

4.37 ± 0.06

45.69 ± 0.06

71.60 ± 3.24

57.07 ± 0.61

 

Sorafenib

 

7.06 ± 0.17

5.45 ± 0.11

19.8 ± 0.12

29.6 ± 0.31

2.81 ± 0.71

  1. (IC50, µM)a values were determined by MTT assay.
  2. aData are expressed as the mean ± standard deviation from the dose response curves of at least three independent experiments.
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