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. 2014 Mar 4;57(6):2755–2772. doi: 10.1021/jm500065f

Table 3. Benzothiazoles Derivatives Synthesized and Evaluated as CK-1δ Inhibitors.

graphic file with name jm-2014-00065f_0013.jpg

compd X Z Y R1 R2 R3 R4 %inh @10 μM (%) CK-1δ IC50 (μM)
MR-3.15 NH CO CH2 H H Cl H >60 0.85 ± 0.10
9 O CO CH2 H H H Cl 20  
10 NH CO   CF3 OMe H H 25  
11 NH CH2 CH2 CF3 OMe H H 25  
12 NH CO CHPh H H H H >60 1.96 ± 0.83
13 NH CO CHPh OEt H H H >60 2.82 ± 0.43
14 NH CO CH2CH2 H H Cl H >60 3.58 ± 0.21
15 NH CO CH2CHPh H H H H >60 2.50 ± 0.33
16 NH CO NH CF3 H H OMe >60 5.50 ± 0.11