892550-43-5Relevant articles and documents
Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors
Cote, Bernard,Boulet, Louise,Brideau, Christine,Claveau, David,Ethier, Diane,Frenette, Richard,Gagnon, Marc,Giroux, Andre,Guay, Jocelyne,Guiral, Sebastien,Mancini, Joseph,Martins, Evelyn,Masse, Frederic,Methot, Nathalie,Riendeau, Denis,Rubin, Joel,Xu, Daigen,Yu, Hongping,Ducharme, Yves,Friesen, Richard W.
, p. 6816 - 6820 (2007)
Phenanthrene imidazole 3 (MF63) has been identified as a novel potent, selective, and orally active mPGES-1 inhibitor. This new series was developed by lead optimization of a hit from an internal HTS campaign. Compound 3 is significantly more potent than the previously reported indole carboxylic acid 1 with an A549 whole cell IC50 of 0.42 μM (50% FBS) and a human whole blood IC50 of 1.3 μM. It exhibited a significant analgesic effect in a guinea pig hyperalgesia model when orally dosed at 30 and 100 mg/kg.
METHODS FOR TREATING OR PREVENTING NEOPLASIAS
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Page/Page column 43, (2008/06/13)
The present invention is directed to a method for treating or preventing a neoplasia in a human patient in need of such treatment comprising administering to the patient a compound that inhibits microsomal prostaglandin E synthase-1 in an amount that is effective for treating or preventing the neoplasia.