4-N-Hydroxy-4-[1-(sulfonyl)piperidin-4-yl]-butyramides as HDAC inhibitors |
| |
Authors: | Rossi Cristina Fincham Christopher I D'Andrea Piero Porcelloni Marina Ettorre Alessandro Mauro Sandro Bigioni Mario Binaschi Monica Maggi Carlo A Nardelli Federica Parlani Massimo Fattori Daniela |
| |
Institution: | Menarini Ricerche Pomezia, via Tito Speri 10, 00040 Pomezia, Rome, Italy. |
| |
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. |
| |
Keywords: | HDAC Cancer Lead optimization |
本文献已被 ScienceDirect PubMed 等数据库收录! |