Application In Synthesis of 1-Boc-4-(Aminomethyl)piperidine. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Discovery of novel tetrahydrobenzo[b]thiophene-3-carbonitriles as histone deacetylase inhibitors. Author is Gediya, Piyush; Vyas, Vivek K.; Carafa, Vincenzo; Sitwala, Nikum; Della Torre, Laura; Poziello, Angelita; Kurohara, Takashi; Suzuki, Takayoshi; Sanna, Vinod; Raguraman, Varalakshmi; Suthindhiran, K.; Ghosh, Debarpan; Bhatia, Dhiraj; Altucci, Lucia; Ghate, Manjunath D..
The discovery and development of isoform-selective histone deacetylase (HDAC) inhibitor is a challenging task because of the sequence homol. among HDAC enzymes. In the present work, novel tetrahydro benzo[b]thiophene-3-carbonitrile based benzamides were designed, synthesized, and evaluated as HDAC inhibitors. Pharmacophore modeling was the main design strategy, and two novel series of tetrahydro benzo[b]thiophene-3-carbonitrile derivatives with piperidine linker (series 1) and piperazine linker (series 2) were identified as HDAC inhibitors. Among all the synthesized compounds, I with 4-(aminomethyl) piperidine linker and II with piperazine linker demonstrated good activity against human HDAC1 and HDAC6, resp. Both the compounds also exhibited good antiproliferative activity against several human cancer cell lines. Both these compounds (I and II) also induced cell cycle arrest and apoptosis in U937 and MDA-MB-231 cancer cells. Overall, for the first time, this research discovered potent isoform-selective HDAC inhibitors using cyclic linker instead of the aliphatic chain and aromatic ring system, which were reported in known HDAC inhibitors.
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Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem