1305197-29-8Relevant articles and documents
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
, 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.