AI Article Synopsis
- Research on alpha(V)beta(3)-receptor antagonists focused on a specific scaffold, N(1)-substituted 4-amino-1H-pyrimidin-2-one.
- The most effective compounds showed IC(50) values in the nano- to subnanomolar range while being highly selective against similar integrins like alpha(IIb)beta(3).
- Some of the compounds were tested in cellular assays, demonstrating their efficacy in practical applications.
Article 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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| http://dx.doi.org/10.1016/s0960-894x(02)00931-9 | DOI Listing |
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