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

…, K Fujimoto, Y Matsumura, A Aoyama, T Harada…

Index: Hoshina, Yoichiro; Ikegami, Satoru; Okuyama, Akihiko; Fukui, Hideto; Inoguchi, Kiyoshi; Maruyama, Tatsuya; Fujimoto, Kyoko; Matsumura, Yuzuru; Aoyama, Akinori; Harada, Tatsuhiro; Tanaka, Hiroshi; Nakamura, Tsutomu Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 1 p. 217 - 220

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Citation Number: 11

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 IC50 of 1.7 nM, and has good pharmacokinetics and oral bioavailability.