Synthesis and Biological Evaluation of N-Hydroxyphenylacrylamides and N-Hydroxypyridin-2-ylacrylamides as Novel Histone Deacetylase Inhibitors was written by Thaler, Florian;Colombo, Andrea;Mai, Antonello;Amici, Raffaella;Bigogno, Chiara;Boggio, Roberto;Cappa, Anna;Carrara, Simone;Cataudella, Tiziana;Fusar, Fulvia;Gianti, Eleonora;di Ventimiglia, Samuele Joppolo;Moroni, Maurizio;Munari, Davide;Pain, Gilles;Regalia, Nickolas;Sartori, Luca;Vultaggio, Stefania;Dondio, Giulio;Gagliardi, Stefania;Minucci, Saverio;Mercurio, Ciro;Varasi, Mario. And the article was included in Journal of Medicinal Chemistry in 2010.Quality Control of 2-Bromopyridine-4-methanol This article mentions the following:
The histone deacetylases (HDACs) are able to regulate gene expression, and histone deacetylase inhibitors (HDACi) emerged as a new class of agents in the treatment of cancer as well as other human disorders such as neurodegenerative diseases. In the present investigation, we report on the synthesis and biol. evaluation of compounds derived from the expansion of a HDAC inhibitor scaffold having N-hydroxy-3-phenyl-2-propenamide and N-hydroxy-3-(pyridin-2-yl)-2-propenamide as core structures and containing a phenyloxopropenyl moiety, either unsubstituted or substituted by a 4-methylpiperazin-1-yl or 4-methylpiperazin-1-ylmethyl group. The compounds were evaluated for their ability to inhibit nuclear HDACs, as well as for their in vitro antiproliferative activity. Moreover, their metabolic stability in microsomes and aqueous solubility were studied and selected compounds were further characterized by in vivo pharmacokinetic experiments These compounds showed a remarkable stability in vivo, compared to hydroxamic acid HDAC inhibitors that have already entered clin. trials. The representative compound I showed in vivo antitumor activity in a human colon carcinoma xenograft model. In the experiment, the researchers used many compounds, for example, 2-Bromopyridine-4-methanol (cas: 118289-16-0Quality Control of 2-Bromopyridine-4-methanol).
2-Bromopyridine-4-methanol (cas: 118289-16-0) belongs to alcohols. A strong base can deprotonate an alcohol to yield an alkoxide ion (R―O−). For example, sodamide (NaNH2), a very strong base, abstracts the hydrogen atom of an alcohol. Grignard and organolithium reagents are powerful tools for organic synthesis, and the most common products of their reactions are alcohols.Quality Control of 2-Bromopyridine-4-methanol
Referemce:
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