European Journal of Medicinal Chemistry p. 53 - 67 (2016)
Update date:2022-08-15
Topics:
Thaler, Florian
Moretti, Loris
Amici, Raffaella
Abate, Agnese
Colombo, Andrea
Carenzi, Giacomo
Fulco, Maria Carmela
Boggio, Roberto
Dondio, Giulio
Gagliardi, Stefania
Minucci, Saverio
Sartori, Luca
Varasi, Mario
Mercurio, Ciro
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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