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) …
MSS Palanki, PE Erdman, LM Gayo-Fung…
Index: Palanki; Erdman; Gayo-Fung; Shevlin; Sullivan; Goldman; Ransone; Bennett; Manning; Suto Journal of medicinal chemistry, 2000 , vol. 43, # 21 p. 3995 - 4004
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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 ...