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Table 1 In vitro cytotoxic activities of the compounds against human cancer cell lines and normal cells

From: Nicotinamide-based diamides derivatives as potential cytotoxic agents: synthesis and biological evaluation

Entry

Compd

no.

Substituents

In vitro cytotoxicity IC a50 (μg/mL)

R1

R2

X

Z

Ar

NCI-H460

A549

NCI-H1975

HL-7702

MDCK

1

4a

H

H

N

CH

3-CF3Ph

> 40

> 40

> 40

> 40

> 40

2

4b

H

CH3

N

CH

3-CF3Ph

36.68 ± 2.80

> 40

> 40

> 40

> 40

3

4c

H

CH3CH(OH)CH2

N

CH

3-CF3Ph

20.63 ± 1.37

26.31 ± 3.22

27.25 ± 2.76

19.73 ± 0.45

16.98 ± 0.84

4

4d

H

CH3COCH2

N

CH

3-CF3Ph

4.07 ± 1.30

13.09 ± 2.45

12.82 ± 1.59

26.87 ± 0.95

13.45 ± 0.29

5

4e

3-CH3-5-Cl

H

C

N

3-CF3Ph

> 40

> 40

> 40

> 40

> 40

6

4f

3-CH3-5-Cl

CH3

C

N

3-CF3Ph

> 40

> 40

> 40

> 40

> 40

7

4g

H

H

N

N

3-CF3Ph

9.17 ± 2.02

20.12 ± 0.48

10.85 ± 2.22

9.86 ± 0.34

13.04 ± 1.27

8

4h

H

CH3

N

N

3-CF3Ph

9.31 ± 2.66

17.18 ± 3.40

12.44 ± 2.52

11.62 ± 2.08

11.06 ± 0.24

9

4i

H

CH3CH(OH)CH2

N

N

3-CF3Ph

13.08 ± 4.49

16.53 ± 3.53

9.15 ± 1.64

14.51 ± 2.19

11.62 ± 0.06

10

4j

4,5-(CH=CH–CH=CH)–

H

CH

N

3-CF3Ph

38.44 ± 3.95

24.79 ± 3.00

25.20 ± 3.35

18.09 ± 1.63

14.30 ± 0.66

11

4k

4,5-(CH=CH–CH=CH)–

CH3

CH

N

3-CF3Ph

> 40

35.30 ± 2.19

> 40

> 40

> 40

12

4l

3-CH3-5-Cl

H

C

CH

3-CF3Ph

> 40

> 40

> 40

> 40

> 40

13

4m

3-CH3-5-Cl

CH3

C

CH

3-CF3Ph

6.85 ± 0.23

6.77 ± 0.86

10.83 ± 1.02

21.44 ± 1.79

21.25 ± 3.59

14

4n

4,5-(CH=CH–CH=CH)–

H

CH

CH

3-CF3Ph

> 40

> 40

> 40

> 40

14.44 ± 0.01

15

4o

4,5-(CH=CH–CH=CH)–

CH3

CH

CH

3-CF3Ph

> 40

> 40

> 40

> 40

> 40

16

5-FU b

8.02 ± 2.35

37.51 ± 3.25

24.75 ± 5.80

11.35 ± 1.67

8.65 ± 0.81

  1. NCI-H460 human large cell lung cancer cell line, A549 human lung cancer cell line, NCI-H1975 human lung cancer cell line, HL-7702 human normal liver cells, MDCK Madin-Darby canine kidney cells
  2. aIC50 compound concentration required to inhibit tumor cell proliferation by 50%
  3. b5-Fluorouracil, used as a positive control