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Table 3 VEGFR-2 inhibitory activity of the synthesized 2,5-disubstituted benzimidazole derivatives 8a-u at 10 µM in reference to sorafenib (I)

From: Receptor-based pharmacophore modeling, molecular docking, synthesis and biological evaluation of novel VEGFR-2, FGFR-1, and BRAF multi-kinase inhibitors

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ID

R1

R2

% Inhibition

8a

H

2-OH

43.03 ± 2.32

8b

H

3-OH

23.82 ± 1.47

8c

H

3-OMe

18.52 ± 0.95

8d

H

2-OH, 3-OMe

53.80 ± 2.62

8e

H

3-OH, 4-OMe

36.36 ± 1.91

8f

H

2,5-OMe

58.29 ± 2.98

8g

H

3,4,5-OMe

47.91 ± 3.53

8h

OMe

2-OH

62.88 ± 3.89

8i

OMe

3-OH

45.16 ± 2.22

8j

OMe

3-OMe

15.67 ± 1.41

8k

OMe

2-OH, 3-OMe

69.50 ± 4.37

8l

OMe

3-OH, 4-OMe

50.62 ± 5.29

8m

OMe

2,5-OMe

6.67 ± 0.08

8n

OMe

3,4,5-OMe

20.81 ± 1.78

8o

Cl

2-OH

22.30 ± 1.95

8p

Cl

3-OH

22.32 ± 0.86

8q

Cl

3-OMe

21.49 ± 1.54

8r

Cl

2-OH, 3-OMe

25.71 ± 1.87

8s

Cl

3-OH, 4-OMe

26.72 ± 1.83

8t

Cl

2,5-OMe

33.99 ± 2.57

8u

Cl

3,4,5-OMe

80.0 ± 3.98

Sorafenib (I)

–

–

99 ± 0.50

  1. Mean % inhibition (duplicate test) at a single dose (10 μM). Data are represented as mean value ± SD
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BMC Chemistry

ISSN: 2661-801X

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