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. Author manuscript; available in PMC: 2017 Apr 28.
Published in final edited form as: J Med Chem. 2015 Nov 9;59(8):3609–3634. doi: 10.1021/acs.jmedchem.5b01457

Table 12. Pyrazolopyrimidine derivatives from Teijin Pharma and BioFocus.

graphic file with name nihms-735690-t0110.jpg
Compd R R1 R2 IC50a (nM)
84 graphic file with name nihms-735690-t0111.jpg H graphic file with name nihms-735690-t0112.jpg 1300
85 graphic file with name nihms-735690-t0113.jpg Me graphic file with name nihms-735690-t0114.jpg 400
rac-86 graphic file with name nihms-735690-t0115.jpg H graphic file with name nihms-735690-t0116.jpg 40
87, TEI-I01800b graphic file with name nihms-735690-t0117.jpg Me graphic file with name nihms-735690-t0118.jpg 130
88b graphic file with name nihms-735690-t0119.jpg Me graphic file with name nihms-735690-t0120.jpg 57
89b graphic file with name nihms-735690-t0121.jpg Me graphic file with name nihms-735690-t0122.jpg 76
90b graphic file with name nihms-735690-t0123.jpg Me graphic file with name nihms-735690-t0124.jpg 54
91, TEI-L03090 4700
a

Expressed as the inhibition of MK2 activity toward a peptide substrate.

b

Compounds 87-90 were in their (S)-configuration.