title: Small molecule biaryl FSH receptor agonists. Part 2: Lead optimization via parallel synthesis.
abstract: Potent small molecule biaryl diketopiperazine FSH receptor agonists such as 10c (EC(50)=13 nM) and 11f (EC(50)=1.2 nM) were discovered through the design, synthesis and evaluation of three biaryl diketopiperazine optimization libraries with over 300 compounds. These libraries were prepared via solid-phase parallel synthesis using a cyclization-release method.
authors.affiliation: Pharmacopeia, Inc, PO Box 5350, Princeton, NJ 08543-5350, USA. tguo@pharmacop.com
authors.forename: Tao
authors.initials: T
authors.lastname: Guo
authors.forename: Anton E P
authors.initials: AE
authors.lastname: Adang
authors.forename: Guizhen
authors.initials: G
authors.lastname: Dong
authors.forename: Dan
authors.initials: D
authors.lastname: Fitzpatrick
authors.forename: Peng
authors.initials: P
authors.lastname: Geng
authors.forename: Koc-Kan
authors.initials: KK
authors.lastname: Ho
authors.forename: Charles H
authors.initials: CH
authors.lastname: Jibilian
authors.forename: Steven G
authors.initials: SG
authors.lastname: Kultgen
authors.forename: Ruiyan
authors.initials: R
authors.lastname: Liu
authors.forename: Edward
authors.initials: E
authors.lastname: McDonald
authors.forename: Kurt W
authors.initials: KW
authors.lastname: Saionz
authors.forename: Kenneth J
authors.initials: KJ
authors.lastname: Valenzano
authors.forename: Nicole C R
authors.initials: NC
authors.lastname: van Straten
authors.forename: Dan
authors.initials: D
authors.lastname: Xie
authors.forename: Maria L
authors.initials: ML
authors.lastname: Webb
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D010879:Piperazines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D011962:Receptors, FSH / Q000819:agonists* / Q000378:metabolism
chemical_list: D010879:Piperazines; D011962:Receptors, FSH