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  • Title: Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.
    Author: Thaler F, Moretti L, Amici R, Abate A, Colombo A, Carenzi G, Fulco MC, Boggio R, Dondio G, Gagliardi S, Minucci S, Sartori L, Varasi M, Mercurio C.
    Journal: Eur J Med Chem; 2016 Jan 27; 108():53-67. PubMed ID: 26629860.
    Abstract:
    In the last decades, inhibitors of histone deacetylases (HDAC) have become an important class of anti-cancer agents. In a previous study we described the synthesis of spiro[chromane-2,4'-piperidine]hydroxamic acid derivatives able to inhibit histone deacetylase enzymes. Herein, we present our exploration for new derivatives by replacing the piperidine moiety with various cycloamines. The goal was to obtain highly potent compounds with a good in vitro ADME profile. In addition, molecular modeling studies unravelled the binding mode of these inhibitors.
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