Tricyclic pharmacophore-based molecules as novel integrin α v β 3 antagonists. Part IV: Preliminary control of α v β 3 selectivity by meta-oriented substitution

…, N Yahata, S Murakami, K Fujishima, M Kitakaze…

Index: Kubota, Dai; Ishikawa, Minoru; Ishikawa, Midori; Yahata, Naokazu; Murakami, Shoichi; Fujishima, Kazuyuki; Kitakaze, Masafumi; Ajito, Keiichi Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 12 p. 4158 - 4181

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Citation Number: 13

Abstract

To establish the in vivo efficacy of αvβ3/αIIbβ3 dual antagonists possessing a tricyclic pharmacophore, a corresponding αvβ3-selective antagonist was required as a control. We initially took two synthetic approaches to obtain αvβ3-selective antagonists based on the RGD recognition pattern or on modification of the dihedral angle between the central benzene ring and the adjacent heterocycle, but both proved unsuccessful. However, ...