RGD mimetics containing phthalimidine fragment as novel ligands of fibrinogen receptor.

Autor: Krysko AA; A.V. Bogatsky Physico-Chemical Institute of the National Academy of Sciences of Ukraine, Lustdorfskaya doroga 86, Odessa 65080, Ukraine. peptides@paco.net, Samoylenko GV, Polishchuk PG, Andronati SA, Kabanova TA, Khristova TM, Kuz'min VE, Kabanov VM, Krysko OL, Varnek AA, Grygorash RY
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Oct 01; Vol. 21 (19), pp. 5971-4. Date of Electronic Publication: 2011 Jul 26.
DOI: 10.1016/j.bmcl.2011.07.063
Abstrakt: 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 α(IIb)β(3) integrin in a suspension of washed human platelets. The key α(IIb)β(3) protein-ligand interactions were determined in docking experiments.
(Copyright © 2011 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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