Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors was written by Oyallon, Bruno;Brachet-Botineau, Marie;Loge, Cedric;Bonnet, Pascal;Souab, Mohamed;Robert, Thomas;Ruchaud, Sandrine;Bach, Stephane;Berthelot, Pascal;Gouilleux, Fabrice;Viaud-Massuard, Marie-Claude;Denevault-Sabourin, Caroline. And the article was included in European Journal of Medicinal Chemistry in 2018.Formula: C11H9ClN2O2 This article mentions the following:
We identified a new series of quinoxaline-2-carboxylic acid derivatives, targeting the human proviral integration site for Moloney murine leukemia virus-1 (HsPim-1) kinase. Seventeen analogs were synthesized providing useful insight into structure-activity relationships studied. Docking studies realized in the ATP pocket of HsPim-1 are consistent with an unclassical binding mode of these inhibitors. The lead compound I was able to block HsPim-1 enzymic activity at nanomolar concentrations (IC50 of 74 nM), with a good selectivity profile against a panel of mammalian protein kinases. In vitro studies on the human chronic myeloid leukemia cell line KU812 showed an antitumor activity at micromolar concentrations As a result, compound I represents a promising lead for the design of novel anticancer targeted therapies. In the experiment, the researchers used many compounds, for example, Ethyl 3-chloroquinoxaline-2-carboxylate (cas: 49679-45-0Formula: C11H9ClN2O2).
Ethyl 3-chloroquinoxaline-2-carboxylate (cas: 49679-45-0) belongs to quinoxaline derivatives. Quinoxaline is isomeric with other naphthyridines including quinazoline, phthalazine and cinnoline. Quinoxaline-1,4-di-N-oxide derivatives have shown to improve the biological results and are endowed with anti-viral, anti-cancer, anti-bacterial, and anti-protozoal activities with application in many other therapeutic areas.Formula: C11H9ClN2O2
Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider