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ID: ALA1144264
Journal: Bioorg Med Chem Lett
Title: Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP(3) antagonists.
Authors: Belley M, Gallant M, Roy B, Houde K, Lachance N, Labelle M, Trimble LA, Chauret N, Li C, Sawyer N, Tremblay N, Lamontagne S, Carrière MC, Denis D, Greig GM, Slipetz D, Metters KM, Gordon R, Chan CC, Zamboni RJ.
Abstract: A series of novel ortho-substituted cinnamic acids have been synthesized, and their binding activity and selectivity on the four prostaglandin E(2) receptors evaluated. Many of them are very potent and selective EP(3) antagonists (K(i) 3-10 nM), while compound 9 is a very good and selective EP(2) agonist (K(i) 8 nM). The biological profile of the EP(2) agonist 9 in vivo and the metabolic profile of selected EP(3) antagonists are also reported.
CiteXplore: 15664806