title: Design and synthesis of potent and selective inhibitors of integrin VLA-4.
abstract: The synthesis and identification of a novel series of inhibitors of integrin VLA-4 are described. Their in vitro activity and selectivity against closely related integrins are also presented.
authors.affiliation: Novartis Institute for Biomedical Research, Novartis Pharmaceuticals Corporation, 556 Morris Avenue, Summit, NJ 07901, USA. sompong.wattanasin@pharma.novartis.com
authors.forename: S
authors.initials: S
authors.lastname: Wattanasin
authors.forename: B
authors.initials: B
authors.lastname: Weidmann
authors.forename: D
authors.initials: D
authors.lastname: Roche
authors.forename: S
authors.initials: S
authors.lastname: Myers
authors.forename: A
authors.initials: A
authors.lastname: Xing
authors.forename: Q
authors.initials: Q
authors.lastname: Guo
authors.forename: M
authors.initials: M
authors.lastname: Sabio
authors.forename: P
authors.initials: P
authors.lastname: von Matt
authors.forename: R
authors.initials: R
authors.lastname: Hugo
authors.forename: S
authors.initials: S
authors.lastname: Maida
authors.forename: P
authors.initials: P
authors.lastname: Lake
authors.forename: M
authors.initials: M
authors.lastname: Weetall
mesh_terms: D018926:Anti-Allergic Agents / Q000037:antagonists & inhibitors*; D015195:Drug Design; D039041:Integrin alpha4beta1; D016023:Integrins / Q000037:antagonists & inhibitors*; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D016201:Receptors, Lymphocyte Homing / Q000037:antagonists & inhibitors*; D016029:Receptors, Very Late Antigen / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014508:Urea / Q000737:chemistry
chemical_list: D018926:Anti-Allergic Agents; D039041:Integrin alpha4beta1; D016023:Integrins; D010455:Peptides; D016201:Receptors, Lymphocyte Homing; D016029:Receptors, Very Late Antigen; D014508:Urea