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

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

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

doi

10.1016/j.ejmech.2015.11.010

subject

Has Abstract

pub_date

2016-01-27 00:00:00

pages

53-67

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(15)30347-0

journal_volume

108

pub_type

杂志文章

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