2. Academic Validation
  3. 2,3-Diphenylpropionic acids as potent VLA-4 antagonists

2,3-Diphenylpropionic acids as potent VLA-4 antagonists

  • Bioorg Med Chem Lett. 2005 Jan 3;15(1):217-20. doi: 10.1016/j.bmcl.2004.09.089.
Yoichiro Hoshina 1,  Satoru Ikegami,  Akihiko Okuyama,  Hideto Fukui,  Kiyoshi Inoguchi,  Tatsuya Maruyama,  Kyoko Fujimoto,  Yuzuru Matsumura,  Akinori Aoyama,  Tatsuhiro Harada,  Hiroshi Tanaka,  Tsutomu Nakamura
Affiliations

Affiliation

  • 1 Central Research Laboratories, Kaken Pharmaceutical Co. Ltd, 14 Shinomiya-minamikawara, Yamashina, Kyoto 607-8042, Japan.
PMID: 15582442 DOI: 10.1016/j.bmcl.2004.09.089
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.

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