Skip to main content
. 2011 Jul 28;2(10):758–763. doi: 10.1021/ml2001455

Table 2. Inhibition of p38α and PBMC Cytokine Release by 5-(2,6-Dichlorophenyl)-2-(arylthio)-6H-pyrimido[1,6-b]pyridazin-6-ones.

graphic file with name ml-2011-001455_0007.jpg

compd R5 R6 R7 p38α IC50 (μM) PBMC IL-1β IC50 (μM) PBMC TNFα IC50 (μM)
21 H H H 0.25 0.40 0.45
22 H H Me 1.4 0.37 0.87
23 H H F 0.123 0.099 0.293
24 H F H 0.45 0.44 0.72
25 H Cl H 0.28 0.35 0.90
26 H Me H 1.4 0.21 0.28
27 Et H H 0.75 0.98 2.8
28 Me H H 0.20 0.33 3.7
29 OH H H 0.36 0.14 0.49
30 H Cl Cl 0.8 0.97 1.2
31 H Me Me 1.9 2.4 3.5
32 H Cl F 0.5 0.18 0.48
33 NH2 H F 0.22 0.28 1.2
34 Cl H F 0.036 0.053 0.275
3 F H F 0.009 0.045 0.051
35 Me H Cl 0.18 0.18 0.16
36 Me H Me 0.26 0.69 0.32