Identification of N-acylhydrazone derivatives as novel lactate dehydrogenase A inhibitors was written by Rupiani, Sebastiano;Buonfiglio, Rosa;Manerba, Marcella;Di Ianni, Lorenza;Vettraino, Marina;Giacomini, Elisa;Masetti, Matteo;Falchi, Federico;Di Stefano, Giuseppina;Roberti, Marinella;Recanatini, Maurizio. And the article was included in European Journal of Medicinal Chemistry in 2015.SDS of cas: 881676-32-0 This article mentions the following:
Glycolysis is drastically increased in tumors and it is the main route to energy production with a minor use of oxidative phosphorylation. Among the key enzymes in the glycolytic process, LDH is emerging as one of the most interesting targets for the development of new inhibitors. In this context, in the present work, we carried out a virtual screening procedure followed by chem. modifications of the identified structures according to a “hit-to-lead” process. The effects of the new mols. were preliminary probed against purified human LDH-A. The compounds active at low micromolar level were addnl. characterized for their activity on some cellular metabolic processes by using Raji human cell line. Within the series, 1 was considered the best candidate, and a more detailed characterization of its biol. properties was performed. In Raji cells exposed to compound 1 we evidenced the occurrence of effects usually observed in cancer cells after LDH-A inhibition: reduced lactate production and NAD/NADH ratio, apoptosis. The flow cytometry anal. of treated cells also showed cell cycle changes compatible with effects exerted at the glycolytic level. Finally, in agreement with the data obtained with other inhibitors or by silencing LDH-A expression, compound 1 was found to increase Raji cells response to some commonly used chemotherapeutic agents. Taken together, all these finding are in support of the LDH-A inhibiting activity of compound 1. In the experiment, the researchers used many compounds, for example, 5-Bromo-1H-pyrrole-3-carbaldehyde (cas: 881676-32-0SDS of cas: 881676-32-0).
5-Bromo-1H-pyrrole-3-carbaldehyde (cas: 881676-32-0) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.SDS of cas: 881676-32-0
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary