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<p>New analogs of <i>N</i>-[4-(methylsulfonyl)-2-nitrophenyl]-1,3-benzodioxol-5-amine (MSNBA), an inhibitor of the intracellular fructose transporter protein GLUT5, were designed using substituent homologation and conformational restriction techniques and synthesized with acceptable yields using standard methods. Primary biotesting demonstrated different abilities of the obtained compounds to inhibit proliferation of K562 chronic myeloid leukemia cells in a fructose-containing medium. All N-substituted MSNBA derivatives were promising for further testing.</p>

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Molecular Design, Synthesis, and Primary Screening of Potential Blockers of the GLUT5 Transporter Protein

  • 期刊论文

  • 发表日期：

    2025年7月1日

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  • E. V. Nurieva,
  • D. A. Shashurin,
  • V. I. Chubinskiy-Nadezhdin,
  • N. A. Zefirov,
  • K. Nasher Ahkami,
  • V. Yu. Vasileva,
  • A. V. Sudarikova,
  • E. R. Milaeva,
  • O. S. Medvedev,
  • O. N. Zefirova

摘要

New analogs of N-[4-(methylsulfonyl)-2-nitrophenyl]-1,3-benzodioxol-5-amine (MSNBA), an inhibitor of the intracellular fructose transporter protein GLUT5, were designed using substituent homologation and conformational restriction techniques and synthesized with acceptable yields using standard methods. Primary biotesting demonstrated different abilities of the obtained compounds to inhibit proliferation of K562 chronic myeloid leukemia cells in a fructose-containing medium. All N-substituted MSNBA derivatives were promising for further testing.