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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 9. Tricyclic and tetracyclic pyrrole derivatives from Novartis.

graphic file with name nihms-735690-t0087.jpg
Compd R IC50a (nM) EC50b (nM)
66 3800
67 graphic file with name nihms-735690-t0088.jpg 1 9
68 graphic file with name nihms-735690-t0089.jpg 15 97 (500)
69 graphic file with name nihms-735690-t0090.jpg 12 260 (700)
70 graphic file with name nihms-735690-t0091.jpg 160 1400 (5800)
a

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

b

Expressed as the ability to inhibit TNFα production in hPBMC cells stimulated with both LPS and IFNγ, and to inhibit Hsp27 phosphorylation in anisomycin-stimulated THP-1 cells (in parentheses).