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Ferrocenyl 2,5-Piperazinediones as Tubulin-Binding Organometallic ABCB1 and ABCG2 Inhibitors Active against MDR Cells.
Wieczorek, Anna; Blauz, Andrzej; Zakrzewski, Janusz; Rychlik, Blazej; Plazuk, Damian.
Afiliación
  • Wieczorek A; Department of Organic Chemistry, Faculty of Chemistry, University of Lódz, Tamka 12, 91-403 Lódz, Poland; Cytometry Lab, Department of Molecular Biophysics, Faculty of Biology and Environmental Protection, University of Lódz, Pomorska 141/143, 90-236 Lódz, Poland.
  • Blauz A; Cytometry Lab, Department of Molecular Biophysics, Faculty of Biology and Environmental Protection, University of Lódz , Pomorska 141/143, 90-236 Lódz, Poland.
  • Zakrzewski J; Department of Organic Chemistry, Faculty of Chemistry, University of Lódz , Tamka 12, 91-403 Lódz, Poland.
  • Rychlik B; Cytometry Lab, Department of Molecular Biophysics, Faculty of Biology and Environmental Protection, University of Lódz , Pomorska 141/143, 90-236 Lódz, Poland.
  • Plazuk D; Department of Organic Chemistry, Faculty of Chemistry, University of Lódz , Tamka 12, 91-403 Lódz, Poland.
ACS Med Chem Lett ; 7(6): 612-7, 2016 Jun 09.
Article en En | MEDLINE | ID: mdl-27326336
The tubulin-microtubule system is a common target of many anticancer drugs. However, the use of chemotherapeutics frequently leads to the development of a clinically relevant phenomenon of multidrug resistance (MDR). One of the basic mechanisms involved in MDR involves elevated expression and/or activity of several ATP-binding cassette superfamily members (ABC transporters) which are normally responsible for the efflux of xenobiotics or secondary metabolites outside the cell. Here we present the synthesis and biological characteristics of ferrocenyl analogues of plinabulin, i.e. one of the so-called "spindle poisons". We found that replacement of the phenyl group of plinabulin by the ferrocenyl moiety turns this compound into a potent inhibitor of ABCB1 and ABCG2, thus making it possible to overcome the multidrug resistance phenomenon. We also demonstrated that the alkyl group attached to the imidazole moiety of ferrocenyl analogues of plinabulin strongly affects their potency to inhibit tubulin polymerization.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2016 Tipo del documento: Article País de afiliación: Polonia Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Med Chem Lett Año: 2016 Tipo del documento: Article País de afiliación: Polonia Pais de publicación: Estados Unidos