| Literature DB >> 15125957 |
Ning Xi1, Stephen Arvedson, Shawn Eisenberg, Nianhe Han, Michael Handley, Liang Huang, Qi Huang, Alexander Kiselyov, Qingyian Liu, Yuelie Lu, Gladys Nunez, Timothy Osslund, David Powers, Andrew S Tasker, Ling Wang, Tingjian Xiang, Shimin Xu, Jiandong Zhang, Jiawang Zhu, Richard Kendall, Celia Dominguez.
Abstract
Novel alphavbeta3 antagonists based on the N-aryl-gamma-lactam scaffold were prepared. SAR studies led to the identification of potent antagonists for alphavbeta3 receptor with excellent selectivity against the structurally related alpha(IIb)beta3 receptor. Additional interactions of N-aryl-gamma-lactam derivatives with alphavbeta3 were found when compared to c(-RGDf[NMe]V-) peptide antagonist. The effects of the conformation and configuration of the gamma-lactam core on the binding were also assessed.Entities:
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Year: 2004 PMID： 15125957 DOI： 10.1016/j.bmcl.2004.03.033
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823