title: 4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors.
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.
authors: Menarini Ricerche Pomezia, via Tito Speri 10, 00040 Pomezia, Rome, Italy.
authors: Cristina
authors: C
authors: Rossi
authors: Christopher I
authors: CI
authors: Fincham
authors: Piero
authors: P
authors: D'Andrea
authors: Marina
authors: M
authors: Porcelloni
authors: Alessandro
authors: A
authors: Ettorre
authors: Sandro
authors: S
authors: Mauro
authors: Mario
authors: M
authors: Bigioni
authors: Monica
authors: M
authors: Binaschi
authors: Carlo A
authors: CA
authors: Maggi
authors: Federica
authors: F
authors: Nardelli
authors: Massimo
authors: M
authors: Parlani
authors: Daniela
authors: D
authors: Fattori
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003110:Colonic Neoplasms / Q000188:drug therapy; D056572:Histone Deacetylase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006655:Histone Deacetylases / Q000378:metabolism*; D006801:Humans; D010880:Piperidines / Q000737:chemistry* / Q000494:pharmacology*; D013450:Sulfones / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D056572:Histone Deacetylase Inhibitors; D010880:Piperidines; D013450:Sulfones; D006655:Histone Deacetylases