title: 2,3-Diphenylpropionic acids as potent VLA-4 antagonists.
abstract: The discovery and SAR of 2,3-diphenylpropionic acid derivatives as highly potent VLA-4 antagonists are described. One representative compound, 9cc has inhibited intercellular adhesion by a VCAM-1/VLA-4 interaction with an IC(50) of 1.7 nM, and has good pharmacokinetics and oral bioavailability.
authors.affiliation: Central Research Laboratories, Kaken Pharmaceutical Co. Ltd, 14 Shinomiya-minamikawara, Yamashina, Kyoto 607-8042, Japan.
authors.forename: Yoichiro
authors.initials: Y
authors.lastname: Hoshina
authors.forename: Satoru
authors.initials: S
authors.lastname: Ikegami
authors.forename: Akihiko
authors.initials: A
authors.lastname: Okuyama
authors.forename: Hideto
authors.initials: H
authors.lastname: Fukui
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Inoguchi
authors.forename: Tatsuya
authors.initials: T
authors.lastname: Maruyama
authors.forename: Kyoko
authors.initials: K
authors.lastname: Fujimoto
authors.forename: Yuzuru
authors.initials: Y
authors.lastname: Matsumura
authors.forename: Akinori
authors.initials: A
authors.lastname: Aoyama
authors.forename: Tatsuhiro
authors.initials: T
authors.lastname: Harada
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Tanaka
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Nakamura
mesh_terms: D000284:Administration, Oral; D001682:Biological Availability; D039041:Integrin alpha4beta1 / Q000037:antagonists & inhibitors*; D011422:Propionates / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D039041:Integrin alpha4beta1; D011422:Propionates; C029658:propionic acid