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Bioinorg Chem Appl. 2017;2017:4736321. doi: 10.1155/2017/4736321. Epub 2017 Jul 19.

Influence of the Number of Axial Bexarotene Ligands on the Cytotoxicity of Pt(IV) Analogs of Oxaliplatin.

Bioinorganic chemistry and applications

Yulia N Nosova, Ilia V Zenin, Varvara P Maximova, Ekaterina M Zhidkova, Kirill I Kirsanov, Ekaterina A Lesovaya, Anna A Lobas, Mikhail V Gorshkov, Olga N Kovaleva, Elena R Milaeva, Markus Galanski, Bernhard K Keppler, Alexey A Nazarov

Affiliations

  1. Department of Medicinal Chemistry and Fine Organic Synthesis, Lomonosov Moscow State University, Leninskie Gory 1/3, Moscow 119991, Russia.
  2. Blokhin Cancer Research Center, 24 Kashirskoye Shosse, Moscow 115478, Russia.
  3. Institute for Energy Problems of Chemical Physics, Russian Academy of Sciences, Leninsky Pr. 38, Bld.2, Moscow 119334, Russia.
  4. I.M. Sechenov First Moscow State Medical University, Moscow, Russia.
  5. Faculty of Chemistry, Institute of Inorganic Chemistry, University of Vienna, Waehringer Str. 42, 1019 Vienna, Austria.

PMID: 28804273 PMCID: PMC5540250 DOI: 10.1155/2017/4736321

Abstract

We present the synthesis and cytotoxic potencies of new Pt(IV) complexes with bexarotene, an anticancer drug that induces cell differentiation and apoptosis via selective activation of retinoid X receptors. In these complexes bexarotene is positioned as an axial ligand. The complex of one bexarotene ligand attached to Pt(IV) oxaliplatin moiety was potent whereas its counterpart carrying two bexarotene ligands was inactive.

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