1296136-93-0Relevant academic research and scientific papers
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
supporting information; experimental part, 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.
Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents
You, Hyun,Youn, Hyung-Seop,Im, Isak,Bae, Man-Ho,Lee, Sang-Kook,Ko, Hyojin,Eom, Soo Hyun,Kim, Yong-Chul
, p. 1153 - 1164 (2011/04/17)
NAmPRTase (PBEF/Visfatin) plays a pivotal role in the salvage pathway of NAD+ biosynthesis. NAmPRTase has been an attractive target for anti-cancer agents that induce apoptosis of tumor cells via a declining plasma NAD+ level. In this report, a series of structural analogs of FK866 (1), a known NAmPRTase inhibitor, was synthesized and tested for inhibitory activities against the proliferation of cancer cells and human NAmPRTase. Among them, compound 7 showed similar anti-cancer and enzyme inhibitory activities to compound 1. Further investigation of compound 7 with X-ray analysis revealed a co-crystal structure in complex with human NAmPRTase, suggesting that Asp219 in the active site of the enzyme could contribute to an additional interaction with the pyrrole nitrogen of compound 7.
