Table 1 In vitro cytotoxic activities (IC50, µM and S.D values) of compounds 5a-f, 9a-c and 10a-c against HCT116, HePG-2, MCF7 and nonmalignant cells WI-38 cell lines. Signifcant values are in bold. aIC50 value is the concentration required to produce 50% inhibition of cancer cell proliferation. Data are presented as the mean ± SD from the dose–response curves of three independent experiments.

From: New oxadiazole and pyrazoline derivatives as anti-proliferative agents targeting EGFR-TK: design, synthesis, biological evaluation and molecular docking study

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Comp.no

R

IC50 (µM)a

HCT116

HePG-2

MCF7

WI-38

5a

benzyl

64.36 ± 3.7

35.58 ± 2.2

78.52 ± 4.1

53.87 ± 3.0

5b

4-Clbenzyl

73.15 ± 4.2

38.13 ± 2.2

84.26 ± 4.4

13.22 ± 1.1

5c

4-CH3benzyl

79.81 ± 4.4

71.38 ± 3.9

92.19 ± 4.9

 > 100

5d

cycloheptyl

88.60 ± 4.8

82.79 ± 4.5

 > 100

46.60 ± 2.7

5e

cyclopentyl

75.58 ± 4.2

59.33 ± 3.4

86.83 ± 4.5

11.71 ± 0.9

5f.

CH2COOCH2CH3

 > 100

91.34 ± 5.0

 > 100

77.31 ± 3.9

9a

3-Br

55.30 ± 3.1

32.58 ± 2.1

46.05 ± 2.5

85.13 ± 4.1

9b

3-NO2

10.19 ± 0.9

7.83 ± 0.5

15.17 ± 1.2

55.91 ± 3.2

9c

3,4-diOCH3

16.18 ± 1.2

12.21 ± 0.9

8.53 ± 0.6

49.61 ± 2.8

10a

3-Br

9.94 ± 0.8

6.32 ± 0.4

8.11 ± 0.6

62.31 ± 3.4

10b

3-NO2

8.73 ± 0.7

3.98 ± 0.2

5.97 ± 0.3

37.94 ± 2.3

10c

3,4-diOCH3

5.55 ± 0.3

1.82 ± 0.1

2.86 ± 0.1

41.17 ± 2.4

DOX

–

5.23 ± 0.3

4.50 ± 0.2

4.17 ± 0.2

6.72 ± 0.5

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