2. Academic Validation
  3. 4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors

4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors

  • Bioorg Med Chem Lett. 2011 Nov 15;21(22):6767-9. doi: 10.1016/j.bmcl.2011.09.042.
Cristina Rossi 1,  Christopher I Fincham,  Piero D'Andrea,  Marina Porcelloni,  Alessandro Ettorre,  Sandro Mauro,  Mario Bigioni,  Monica Binaschi,  Carlo A Maggi,  Federica Nardelli,  Massimo Parlani,  Daniela Fattori
Affiliations

Affiliation

  • 1 Menarini Ricerche Pomezia, via Tito Speri 10, 00040 Pomezia, Rome, Italy.
PMID: 21978679 DOI: 10.1016/j.bmcl.2011.09.042
Abstract

A series of N-substituted 4-alkylpiperidine hydroxamic acids, corresponding to the basic structure of histone deacetylase (HDAC) inhibitors (zinc binding moiety-linker-capping group) has been previously reported by our group. 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. We report here the second part of the strategy used in our research group to find a new class of HDAC inhibitors, namely the SAR study for the compounds bearing a sulfonyl group on the piperidine nitrogen. In the present work, we have considered both sulfonamides and sulfonyl ureas.

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