Inhibitors of NF-κB and AP-1 Gene Expression: SAR Studies on the Pyrimidine Portion of 2-Chloro-4-trifluoromethylpyrimidine-5-[N-(3', 5'-bis (trifluoromethyl) phenyl) …

…, RW Sullivan, ME Goldman, LJ Ransone…

Index: Sullivan, Robert W.; Bigam, Colin G.; Erdman, Paul E.; Palanki, Moorthy S. S.; Anderson, David W.; Goldman, Mark E.; Ransone, Lynn J.; Suto, Mark J. Journal of Medicinal Chemistry, 1998 , vol. 41, # 4 p. 413 - 419

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Citation Number: 61

Abstract

We investigated the structure-activity relationship studies of N-[3, 5-bis (trifluoromethyl) phenyl][2-chloro-4-(trifluoromethyl) pyrimidin-5-yl] carboxamide (1), an inhibitor of transcription mediated by both NF-κB and AP-1 transcription factors, with the goal of improving its potential oral bioavailability. Compounds were examined for cell-based activity, were fit to Lipinski's rule of 5, and were examined for potential gastrointestinal ...