263753-02-2Relevant articles and documents
Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP3 antagonists
Belley, Michel,Gallant, Michel,Roy, Bruno,Houde, Karine,Lachance, Nicolas,Labelle, Marc,Trimble, Laird A.,Chauret, Nathalie,Li, Chun,Sawyer, Nicole,Tremblay, Nathalie,Lamontagne, Sonia,Carriere, Marie-Claude,Denis, Danielle,Greig, Gillian M.,Slipetz, Deborah,Metters, Kathleen M.,Gordon, Robert,Chan, Chi Chung,Zamboni, Robert J.
, p. 527 - 530 (2007/10/03)
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 EP3 antagonists (Ki 3-10 nM), while compound 9 is a very good and selective EP2 agonist (Ki 8 nM). The biological profile of the EP2 agonist 9 in vivo and the metabolic profile of selected EP3 antagonists are also reported.
