Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372584 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
The novel RGD mimetics with phthalimidine central fragment were synthesized with the use of 4-piperidine-4-yl-butyric, 4-piperidine-4-yl-benzoic, 4-piperazine-4-yl-benzoic and 1,2,3,4-tetrahydroisoquinoline-7-carboxylic acids as surrogates of Arg motif. The synthesized compounds potently inhibited platelet aggregation in vitro and blocked FITC-Fg binding to αIIbβ3 integrin in a suspension of washed human platelets. The key αIIbβ3 protein–ligand interactions were determined in docking experiments.
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Related Topics
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Organic Chemistry
Authors
Andrei A. Krysko, Georgiy V. Samoylenko, Pavel G. Polishchuk, Sergei A. Andronati, Tatyana A. Kabanova, Tetiana M. Khristova, Victor E. Kuz’min, Vladimir M. Kabanov, Olga L. Krysko, Alexandre A. Varnek, Ruslan Ya. Grygorash,