910540-11-3Relevant academic research and scientific papers
Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors
Rossi, Cristina,Porcelloni, Marina,D'Andrea, Piero,Fincham, Christopher I.,Ettorre, Alessandro,Mauro, Sandro,Squarcia, Antonella,Bigioni, Mario,Parlani, Massimo,Nardelli, Federica,Binaschi, Monica,Maggi, Carlo A.,Fattori, Daniela
supporting information; experimental part, p. 2305 - 2308 (2011/05/15)
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.
Hydroxamates as Histone Deacetylase Inhibitors and Pharmaceutical Formulations Containing Them
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Page/Page column 6-7, (2008/12/08)
Compounds of structure (I) having histone deacetylase (HDAC) inhibitor activity are described. The compounds are chemically characterised by the presence of hydroxamic acid, with zinc as chelator, and an aromatic nucleus connected by a linker in which either a bicyclic aromatic system or a piperidino ring are present.
HYDROXAMATES AS HISTONE DEACETYLASE INHIBITORS AND PHARMACEUTICAL FORMULATIONS CONTAINING THEM
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Page/Page column 14, (2010/11/23)
Compounds of structure (I) having histone deacetylase (HDAC) inhibitor activity are described. The compounds are chemically characterised by the presence of hydroxamic acid, with zinc as chelator, and an aromatic nucleus connected by a linker in which eit
