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<p>Naturally occurring phenols were incorporated into the mycophenolic acid (MPA) core to form sixteen new MPA derivatives. Ester conjugates of MPA with isoeugenol, methyl <i>o</i>-coumarate, and raspberry ketone exhibited the highest antioxidant activity in the DPPH test. These derivatives were then tested against the human pancreatic cancer AsPC-1 cells, showing cytotoxicity similar to that of the referential parent compounds MPA and mycophenolate mofetil (MMF). Subsequently, most of the obtained MPA esters proved activity against the T-Jurkat cells and peripheral blood mononuclear cells (PBMCs), serving as an immunosuppressive model, and worked as inosine-5’-monophosphate dehydrogenase (IMPDH) inhibitors. The most promising immunosuppressive conjugates were the esters of MPA with sesamol and raspberry ketone structural motifs, which held the highest selectivity index (SI) for PBMCs, thus serving as a good starting point for new drug development.</p>

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Direct synthesis of mycophenolic acid aryl esters with antioxidant and antiproliferative properties

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年7月17日

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  • Juliusz Walczak,
  • Dorota Iwaszkiewicz-Grześ,
  • Magdalena Śliwka-Kaszyńska,
  • Agnieszka Kurdyn,
  • Ewa Augustin,
  • Agnieszka Viapiana,
  • Alina Plenis,
  • Grzegorz Cholewiński

摘要

Naturally occurring phenols were incorporated into the mycophenolic acid (MPA) core to form sixteen new MPA derivatives. Ester conjugates of MPA with isoeugenol, methyl o-coumarate, and raspberry ketone exhibited the highest antioxidant activity in the DPPH test. These derivatives were then tested against the human pancreatic cancer AsPC-1 cells, showing cytotoxicity similar to that of the referential parent compounds MPA and mycophenolate mofetil (MMF). Subsequently, most of the obtained MPA esters proved activity against the T-Jurkat cells and peripheral blood mononuclear cells (PBMCs), serving as an immunosuppressive model, and worked as inosine-5’-monophosphate dehydrogenase (IMPDH) inhibitors. The most promising immunosuppressive conjugates were the esters of MPA with sesamol and raspberry ketone structural motifs, which held the highest selectivity index (SI) for PBMCs, thus serving as a good starting point for new drug development.