title: Lead optimisation of the N1 substituent of a novel series of indazole arylsulfonamides as CCR4 antagonists and identification of a candidate for clinical investigation.
abstract: Synthesis and preliminary SAR of the N1 substituent of a novel series of indazole sulfonamide chemokine receptor 4 (CCR4) antagonist is reported. Compound 7r was identified for further development.
authors.affiliation: Department of Medicinal Chemistry, Respiratory CEDD, GlaxoSmithKline Medicines Research Centre, Stevenage, Hertfordshire, United Kingdom. pan.a.procopiou@gsk.com
authors.forename: Panayiotis A
authors.initials: PA
authors.lastname: Procopiou
authors.forename: Alison J
authors.initials: AJ
authors.lastname: Ford
authors.forename: Rebecca H
authors.initials: RH
authors.lastname: Graves
authors.forename: David A
authors.initials: DA
authors.lastname: Hall
authors.forename: Simon T
authors.initials: ST
authors.lastname: Hodgson
authors.forename: Yannick M L
authors.initials: YM
authors.lastname: Lacroix
authors.forename: Deborah
authors.initials: D
authors.lastname: Needham
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Slack
mesh_terms: D006801:Humans; D007191:Indazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011485:Protein Binding / Q000187:drug effects; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D007191:Indazoles; D019707:Receptors, Chemokine; D013449:Sulfonamides