Alkyl piperidine and piperazine hydroxamic acids as HDAC inhibitors |
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Authors: | 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 |
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Affiliation: | a Menarini Ricerche Pomezia, via Tito Speri 10, 00040 Pomezia, Rome, Italy b Menarini Ricerche Firenze, via Rismondo 12A, 50131 Florence, Italy |
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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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Keywords: | HDAC Cancer Lead finding |
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