Highly potent and selective alphaVbeta3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones |
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| Authors: | Zechel Christian Backfisch Gisela Delzer Jürgen Geneste Hervé Graef Claudia Hornberger Wilfried Kling Andreas Lange Udo E W Lauterbach Arnulf Seitz Werner Subkowski Thomas |
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| Institution: | BASF AG, D-67056 Ludwigshafen, Germany. zechel_christian@lilly.com |
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| Abstract: | 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. |
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