Title |
Synthesis, biological characterization and molecular modeling insights of spirochromanes as potent HDAC inhibitors
|
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Published in |
European Journal of Medicinal Chemistry, November 2015
|
DOI | 10.1016/j.ejmech.2015.11.010 |
Pubmed ID | |
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 |
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. |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 22 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 7 | 32% |
Other | 3 | 14% |
Student > Bachelor | 2 | 9% |
Student > Doctoral Student | 2 | 9% |
Researcher | 2 | 9% |
Other | 4 | 18% |
Unknown | 2 | 9% |
Readers by discipline | Count | As % |
---|---|---|
Chemistry | 10 | 45% |
Biochemistry, Genetics and Molecular Biology | 3 | 14% |
Agricultural and Biological Sciences | 2 | 9% |
Environmental Science | 1 | 5% |
Unknown | 6 | 27% |