Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting 伪₅尾₁: Part 1

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• 作者：B&eacute ; n&eacute ; dicte Delouvri&eacute ; ^a ; ^{benedicte.delouvrie@astrazeneca.com} ; Katherine Al-Kadhimi^b ; Jean-Claude Arnould^a ; Simon T. Barry^b ; Darren A.E. Cross^b ; Myriam Didelot^a ; Paul R. Gavine^c ; Herv&eacute ; Germain^a ; Craig S. Harris^a ; Adina M. Hughes^b ; David A. Jude^b ; Jane Kendrew^b ; Christine Lambert-van der Brempt^a ; Jean-Jacques Lohmann^a ; Morgan M&eacute ; nard^a ; Andrew A. Mortlock^b ; Martin Pass^b ; Claire Rooney^b ; Michel Vautier^a ; Jennifer L. Vincent^b ; Nicolas Warin^a
• 关键词：Integrin 伪5尾1 antagonist ; Zwitterion ; RGD integrin ; Angiogenesis
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 June, 2012
• 卷：22
• 期：12
• 页码：4111-4116
• 文件大小：2419 K

摘要

Potent antagonists of the integrin 伪₅尾₁, which are RGD mimetics built from tyrosine are described. This letter describes the optimization of in vitro potency obtained by variation of two parts of the molecule, the basic group and the linker between the basic group and the phenyl central core.