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Synthesis, molecular docking and biological evaluation as HDAC inhibitors of cyclopeptide mimetics by a tandem three-component reaction and intramolecular [3+2] cycloaddition

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Abstract

Novel macrocyclic peptide mimetics have been synthesized by exploiting a three-component reaction and an azide–alkyne [3 + 2] cycloaddition. The prepared compounds were screened as HDAC inhibitors allowing us to identify a new compound with promising biological activity. In order to rationalize the biological results, computational studies have also been performed.

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Authors and Affiliations

  1. Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche and Drug and Food Biotechnology Center, DiSCAFF, Università degli Studi del Piemonte Orientale “A. Avogadro”, Via Bovio 6, 28100, Novara, Italy

    Tracey Pirali, Valeria Faccio, Riccardo Mossetti, Ambra A. Grolla, Armando A. Genazzani & Gian Cesare Tron

  2. Dipartimento di Scienze Farmaceutiche, Università di Salerno, via Ponte Don Melillo, 84084, Fisciano, SA, Italy

    Simone Di Micco & Giuseppe Bifulco

Authors
  1. Tracey Pirali
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  2. Valeria Faccio
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  3. Riccardo Mossetti
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  4. Ambra A. Grolla
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  5. Simone Di Micco
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  6. Giuseppe Bifulco
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  7. Armando A. Genazzani
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  8. Gian Cesare Tron
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Corresponding authors

Correspondence to Giuseppe Bifulco or Gian Cesare Tron.

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Pirali, T., Faccio, V., Mossetti, R. et al. Synthesis, molecular docking and biological evaluation as HDAC inhibitors of cyclopeptide mimetics by a tandem three-component reaction and intramolecular [3+2] cycloaddition. Mol Divers 14, 109–121 (2010). https://doi.org/10.1007/s11030-009-9153-9

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  • DOI: https://doi.org/10.1007/s11030-009-9153-9

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