Tricyclic pharmacophore-based molecules as novel integrin α v β 3 antagonists. Part 2: Synthesis of potent α v β 3/α IIb β 3 dual antagonists

M Ishikawa, D Kubota, M Yamamoto, C Kuroda…

文献索引：Ishikawa, Minoru; Kubota, Dai; Yamamoto, Mikio; Kuroda, Chizuko; Iguchi, Maki; Koyanagi, Akihiro; Murakami, Shoichi; Ajito, Keiichi Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 7 p. 2109 - 2130

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被引用次数: 24

摘要

We synthesized 4-aminopiperidine derivatives of our prototype integrin αvβ3 antagonist 1 in an attempt to increase the activity and water solubility. Introduction of one or two hydrophilic moieties into the central aromatic ring and/or the benzene ring at the C-terminus of 1 increased water solubility and enhanced inhibition of cell adhesion. The results of a structure–activity relationships (SAR) study indicated that the torsion angle between the ...