title: Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.
abstract: Analogs of PGE(2) with introduction of diene groups at the omega-side chain have been synthesized and evaluated for their binding affinity for EP(2) and EP(4) receptors. An optimized analog (compound 9b) showed high potency and selectivity for the EP(4) receptor over other known receptors.
authors.affiliation: Department of Medicinal Chemistry, EMD Serono Research Institute, Inc., Rockland, MA 02370, USA. yufang.xiao@emdserono.com
authors.forename: Yufang
authors.initials: Y
authors.lastname: Xiao
authors.forename: Gian Luca
authors.initials: GL
authors.lastname: Araldi
authors.forename: Zhong
authors.initials: Z
authors.lastname: Zhao
authors.forename: Nadia
authors.initials: N
authors.lastname: Brugger
authors.forename: Srinivasa
authors.initials: S
authors.lastname: Karra
authors.forename: David
authors.initials: D
authors.lastname: Fischer
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Palmer
mesh_terms: D000818:Animals; D002460:Cell Line; D015232:Dinoprostone / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D006207:Half-Life; D006801:Humans; D051381:Rats; D018078:Receptors, Prostaglandin E / Q000819:agonists*; D058307:Receptors, Prostaglandin E, EP2 Subtype; D058309:Receptors, Prostaglandin E, EP4 Subtype
chemical_list: C545644:PTGER2 protein, human; C545650:PTGER4 protein, human; D018078:Receptors, Prostaglandin E; D058307:Receptors, Prostaglandin E, EP2 Subtype; D058309:Receptors, Prostaglandin E, EP4 Subtype; D015232:Dinoprostone