Synthesis, biological evaluation and molecular docking studies of 2-piperazin-1-yl-quinazolines as platelet aggregation inhibitors and ligands of integrin alpha(IIb)beta(3)

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 alpha(IIb)beta(3) integrin in a suspension of washed human platel...

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Published inBioorganic & medicinal chemistry letters Vol. 26; no. 7; pp. 1839 - 1843
Main Authors Krysko, Andrei A., Kornylov, Alexander Yu, Polishchuk, Pavel G., Samoylenko, Georgiy V., Krysko, Olga L., Kabanova, Tatyana A., Kravtsov, Victor Ch, Kabanov, Vladimir M., Wicher, Barbara, Andronati, Sergei A.
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier 01.04.2016
Subjects
Chemistry
Chemistry, Medicinal
Chemistry, Organic
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Physical Sciences
Science & Technology
ALPHA-IIB-BETA-3
2-Piperazin-1-yl-quinazoline
Fibrinogen receptor antagonists
Platelet aggregation
alpha(IIb)beta
ANTAGONISTS
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Summary: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 alpha(IIb)beta(3) integrin in a suspension of washed human platelets. The key alpha(IIb)beta(3) protein-ligand interactions were determined in docking experiments and some correlations have been observed between values of the affinity and docking scores. (C) 2016 Elsevier Ltd. All rights reserved.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2016.02.011