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Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors.

Authors:
Florian Thaler Loris Moretti Raffaella Amici Agnese Abate Andrea Colombo Giacomo Carenzi Maria Carmela Fulco Roberto Boggio Giulio Dondio Stefania Gagliardi Saverio Minucci Luca Sartori Mario Varasi Ciro Mercurio

Eur J Med Chem 2016 Jan 11;108:53-67. Epub 2015 Nov 11.

Genextra Group, DAC Srl, Genextra Group, Via Adamello 16, 20139 Milan, Italy. Electronic address:

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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http://dx.doi.org/10.1016/j.ejmech.2015.11.010DOI Listing
January 2016

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