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Table 1 Various N-Benzothiazolyl-2-Phenyl Acetamide derived compounds with substitutions at the six substitution sites, percentage inhibition showed at a concentration of 10 μM and their IC50 values

From: Novel group-based QSAR and combinatorial design of CK-1δ inhibitors as neuroprotective agents

Compound

R1

R2

R3

R4

R5

R6

IC50

1

H

Me

H

Cl

H

H

0.083

2

H

CF3

H

Cl

H

H

0.023

3

H

OMe

H

Cl

H

H

0.53

4

H

OCF3

H

Cl

H

H

0.54

5

H

OEt

H

Cl

H

H

1.21

6

H

CF3

Cl

H

H

H

0.068

7

H

OMe

Cl

H

H

H

9.71

8

H

OEt

Cl

H

H

H

17.43

9

H

CF3

H

H

Cl

H

0.065

10

H

OMe

H

H

Cl

H

0.75

11

H

OEt

H

H

Cl

H

1.11

12

H

Br

OMe

H

H

H

0.26

13

H

Cl

OMe

H

H

H

0.32

14

H

F

OMe

H

H

H

1.17

15

H

Me

OMe

H

H

H

0.29

16

H

OMe

OMe

H

H

H

2.22

17

H

OCF3

OMe

H

H

H

0.62

18

H

OEt

OMe

H

H

H

5.76

19

H

CF3

H

OMe

H

H

0.042

20

H

OMe

H

OMe

H

H

0.42

21

H

OEt

H

OMe

H

H

0.99

22

H

CF3

H

CF3

H

H

0.087

23

H

CF3

H

H

OMe

H

0.033

24

H

OMe

H

H

OMe

H

0.57

25

H

OEt

H

H

OMe

H

1.09

26

H

H

H

H

H

H

0.33

27

H

CF3

H

H

H

H

0.047

28

H

CF3

H

Cl

Cl

H

0.056

29

H

OMe

H

Cl

Cl

H

1.24

30

H

OEt

H

Cl

Cl

H

3.43

31

H

OCF3

H

Cl

Cl

H

0.59

32

H

CF3

OMe

H

H

OMe

0.19

33

H

OCF3

H

OMe

OMe

OMe

0.079

34

H

OMe

H

OMe

OMe

OMe

1.12

35

H

OEt

H

OMe

OMe

OMe

1.43

36

H

CF3

H

OMe

OMe

OMe

0.015

37

H

H

H

Cl

H

H

0.85