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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| Authors: | Tracey Pirali Valeria Faccio Riccardo Mossetti Ambra A. Grolla Simone Di Micco Giuseppe Bifulco Armando A. Genazzani Gian Cesare Tron |
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| Affiliation: | 1.Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche and Drug and Food Biotechnology Center, DiSCAFF,Università degli Studi del Piemonte Orientale “A. Avogadro”,Novara,Italy;2.Dipartimento di Scienze Farmaceutiche,Università di Salerno,Fisciano,Italy |
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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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