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SM ISO690:2012 KRYSKO, Andrei, KORNYLOV, Alexander Yu., POLISHCHUK, Pavel, SAMOYLENKO, Georgiy, KRYSKO, Olga, KABANOVA, Tatyana, KRAVTSOV, Victor, KABANOV, Vladimir, WICHER, Barbara, ANDRONATI, Sergei. Synthesis, biological evaluation and molecular docking studies of 2-piperazin-1-yl-quinazolines as platelet aggregation inhibitors and ligands of integrin αIIbβ3. In: Bioorganic and Medicinal Chemistry Letters, 2016, vol. 26, pp. 1839-1843. ISSN 0960-894X. DOI: https://doi.org/10.1016/j.bmcl.2016.02.011 |
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Bioorganic and Medicinal Chemistry Letters | |
Volumul 26 / 2016 / ISSN 0960-894X /ISSNe 1464-3405 | |
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DOI:https://doi.org/10.1016/j.bmcl.2016.02.011 | |
Pag. 1839-1843 | |
Rezumat | |
A series of 2-piperazin-1-yl-quinazolines were synthesized and evaluated for their antiaggregative activity. The synthesized small molecule compounds have potently inhibited platelet aggregation in vitro and blocked FITC-Fg binding to αIIbβ3integrin in a suspension of washed human platelets. The key αIIbβ3protein–ligand interactions were determined in docking experiments and some correlations have been observed between values of the affinity and docking scores. |
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Cuvinte-cheie 2-Piperazin-1-yl-quinazoline, Fibrinogen receptor antagonists, Platelet aggregation, αIIbβ3 |
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