Novel potent and selective α v β 3/α v β 5 integrin dual antagonists with reduced binding affinity for human serum albumin

…, CL Manthey, M Chaikin, J Lattanze, C Crysler…

文献索引：Raboisson, Pierre; Manthey, Carl L.; Chaikin, Margery; Lattanze, Jennifer; Crysler, Carl; Leonard, Kristi; Pan, Wenxi; Tomczuk, Bruce E.; Marugan, Juan Jose European Journal of Medicinal Chemistry, 2006 , vol. 41, # 7 p. 847 - 861

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被引用次数: 20

摘要

The binding of lead compounds and drugs to human serum albumin (HSA) is a ubiquitous problem in drug discovery since it modulates the availability of the leads and drugs to their intended target, which is linked to biological efficacy. In our continuing efforts to identify small molecule αVβ3 and αVβ5 dual antagonists, we recently reported indoles 2–4 as potent and selective αVβ3/αVβ5 antagonists with good oral bioavailability profile. In spite of ...