Highly potent and selective αVβ3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones

Autor:	Jürgen Delzer, Wilfried Hornberger, Christian Zechel, Gisela Backfisch, Thomas Subkowski, Andreas Kling, Werner Seitz, Claudia Isabella Graef, Udo E.W Lange, Hervé Geneste, Arnulf Lauterbach
Rok vydání:	2003
Předmět:	Stereochemistry Clinical Biochemistry Integrin Pharmaceutical Science Enzyme-Linked Immunosorbent Assay Pyrimidinones Ligands Guanidines Biochemistry Chemical synthesis Structure-Activity Relationship Solid-phase synthesis Drug Discovery Combinatorial Chemistry Techniques Receptor Molecular Biology biology Chemistry Cell adhesion molecule Molecular Mimicry Organic Chemistry Integrin alphaVbeta3 In vitro biology.protein Molecular Medicine Indicators and Reagents Vitronectin Selectivity
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 13:165-169
ISSN:	0960-894X
Popis:	Solid-phase synthesis and SAR of alpha(V)beta(3)-receptor antagonists based on a N(1)-substituted 4-amino-1H-pyrimidin-2-one scaffold are described. The most potent compounds exhibited IC(50) values towards alpha(V)beta(3) in the nano- to subnanomolar range and high selectivity versus related integrins like alpha(IIb)beta(3). For selected examples efficacy in functional cellular assays was demonstrated.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f46b389f02a87c71234e971349a430b0 https://doi.org/10.1016/s0960-894x(02)00931-9 Zobrazit plný text záznamu Full Text from ScienceDirect