title: Design, synthesis, and evaluation of naphthalene-sulfonamide antagonists of human CCR8.
abstract: The design, synthesis, and structure-activity relationship development of naphthalene-derived human CCR8 antagonists is described. In vitro binding assay results of these investigations are reported, critical interactions of the antagonists with CCR8 are defined, and preliminary physicochemical and pharmacokinetic data for the naphthalene scaffold are presented.
authors.affiliation: Department of Medicinal Chemistry, Department of Pharmacology, and Drug Safety and Disposition, Millennium Pharmaceuticals, 40 Landsdowne Street, Cambridge, Massachusetts 02139, USA. tracy.jenkins@biogenidec.com
authors.forename: Tracy J
authors.initials: TJ
authors.lastname: Jenkins
authors.forename: Bing
authors.initials: B
authors.lastname: Guan
authors.forename: Mingshi
authors.initials: M
authors.lastname: Dai
authors.forename: Gang
authors.initials: G
authors.lastname: Li
authors.forename: Thomas E
authors.initials: TE
authors.lastname: Lightburn
authors.forename: Shan
authors.initials: S
authors.lastname: Huang
authors.forename: B Scott
authors.initials: BS
authors.lastname: Freeze
authors.forename: Douglas F
authors.initials: DF
authors.lastname: Burdi
authors.forename: Swanee
authors.initials: S
authors.lastname: Jacutin-Porte
authors.forename: Robert
authors.initials: R
authors.lastname: Bennett
authors.forename: Weirong
authors.initials: W
authors.lastname: Chen
authors.forename: Charles
authors.initials: C
authors.lastname: Minor
authors.forename: Shomir
authors.initials: S
authors.lastname: Ghosh
authors.forename: Christopher
authors.initials: C
authors.lastname: Blackburn
authors.forename: Kenneth M
authors.initials: KM
authors.lastname: Gigstad
authors.forename: Matthew
authors.initials: M
authors.lastname: Jones
authors.forename: Roland
authors.initials: R
authors.lastname: Kolbeck
authors.forename: Wei
authors.initials: W
authors.lastname: Yin
authors.forename: Sean
authors.initials: S
authors.lastname: Smith
authors.forename: Daniel
authors.initials: D
authors.lastname: Cardillo
authors.forename: Timothy D
authors.initials: TD
authors.lastname: Ocain
authors.forename: Geraldine C
authors.initials: GC
authors.lastname: Harriman
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D001692:Biological Transport; D002118:Calcium / Q000378:metabolism; D002460:Cell Line; D006224:Cricetinae; D003412:Cricetulus; D015195:Drug Design; D006801:Humans; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D054401:Receptors, CCR8; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*; D012995:Solubility; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: C103330:CCR8 protein, human; D009281:Naphthalenes; D054401:Receptors, CCR8; D019707:Receptors, Chemokine; D013449:Sulfonamides; D002118:Calcium