Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371141 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
We report here the strategy used in our research group to find a new class of histone deacetylase (HDAC) inhibitors.A series of N-substituted 4-alkylpiperazine and 4-alkylpiperidine hydroxamic acids, corresponding to the basic structure of HDAC inhibitors (zinc binding moiety-linker-capping group) has been designed, prepared, and tested for HDAC inhibition.Linker length and aromatic capping group connection were systematically varied to find the optimal geometric parameters. A new series of submicromolar inhibitors was thus identified, which showed antiproliferative activity on HCT-116 colon carcinoma cells.
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Organic Chemistry
Authors
Cristina Rossi, Marina Porcelloni, Piero D’Andrea, Christopher I. Fincham, Alessandro Ettorre, Sandro Mauro, Antonella Squarcia, Mario Bigioni, Massimo Parlani, Federica Nardelli, Monica Binaschi, Carlo A. Maggi, Daniela Fattori,