N-Aryl-γ-lactams as integrin αvβ3 antagonists

Autor:	Yuelie Lu, Ling Wang, Michael Handley, Ning Xi, Stephen Arvedson, Andrew Tasker, Jiandong Zhang, Tingjian Xiang, Osslund Timothy D, Celia Dominguez, Qi Huang, Liang Huang, David Powers, Nianhe Han, Gladys Nunez, Qingyian Liu, Jiawang Zhu, Shawn Eisenberg, Shimin Xu, Alexander S. Kiselyov, Richard Kendall
Rok vydání:	2004
Předmět:	chemistry.chemical_classification Stereochemistry Aryl Organic Chemistry Clinical Biochemistry Antagonist Pharmaceutical Science Peptide Biochemistry Chemical synthesis Amidine chemistry.chemical_compound chemistry Drug Discovery Lactam Molecular Medicine Selectivity Receptor Molecular Biology
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 14:2905-2909
ISSN:	0960-894X
Popis:	Novel αvβ3 antagonists based on the N-aryl-γ-lactam scaffold were prepared. SAR studies led to the identification of potent antagonists for αvβ3 receptor with excellent selectivity against the structurally related αIIbβ3 receptor. Additional interactions of N-aryl-γ-lactam derivatives with αvβ3 were found when compared to c(-RGDf[NMe]V-) peptide antagonist. The effects of the conformation and configuration of the γ-lactam core on the binding were also assessed.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::6327503f49e45e3cee545d9f88871868 https://doi.org/10.1016/j.bmcl.2004.03.033 Zobrazit plný text záznamu Full Text from ScienceDirect