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Table 2 Inhibitors of DDX3Original table attached in the e-mail.  Please use this  for the paper. Font and Bold features should be maintained

From: DDX3, a potential target for cancer treatment

Structure for modification

Cmpd #

n

R1

R2

Ki [μM]

Reference

1a

2

2-OH

3-Br

5.4

 

1b

2

2-OH

3-F

0.3

 

1c

2

2-OH

3,5-diF

0.5

 

1d

2

2-OH

3-(O-CH2-O)-4

1.0

[98]

1e

2

2-OH

3,4,5-triOMe

0.1

 

1f

2

2-Cl

3,4,5-triOMe

3.9

 

1 g

2

2-COOH

3-(O-CH2-O)-4

0.4

 

1 h

2

2-COOH

4-OMe

2.0

 

2a

2

2-OH

3-Br

4.2

[98]

2b

2

2-OH

3-F

4.3

 

3

2

2-OH

3-Br

28

[98]

Structure for modification

Cmpd#

n

R1

R2

R3

Ki [μM]

 

4a

0

NH-Ph

H

-

0.4

 

4b

0

morpholinyl

3-Cl

-

1.6

[98]

4c

1

morpholinyl

3-Cl

-

2.9

 

4d

1

NEt2

H

-

0.1

 

5a

0

NH-Ph

H

Ph(4-NHCOCH3)

0.3

 

5b

1

NH-Ph

H

Ph(4-NHCOCH3)

0.5

 

5c

0

morpholinyl

H

Ph(4-NHCOCH3)

2.2

 

5d

0

morpholinyl

F

Ph(2-OH)

0.7

 

5e

1

morpholinyl

H

Ph(2-OH)

0.6

[98]

5f

1

morpholinyl

H

Ph(2-OH, 5-Cl)

1.9

 

5 g

1

morpholinyl

H

Ph(2-OH, 3-NO2)

4.0

 

5 h

0

morpholinyl

4-F

Ph(2-OH)

0.4

 

5i

0

NH-Ph(4-F)

4-F

Ph(2-OH)

0.1

 

5j

0

morpholinyl

4-F

2-methyl-indol-3-yl

0.2

 

6a

0

morpholinyl

4-F

Ph(2-Cl, 4-NO2)

0.3

 

6b

0

piperidinyl

H

Ph(4-Cl)

0.4

[98]

Structure modification

Compound Name

 

RK-33

[47]

ZINC00011012

[104]