From Synthetic Simplified Marine Metabolite Analogues to New Selective Allosteric Inhibitor of Aurora B Kinase was written by Juillet, Charlotte;Ermolenko, Ludmila;Boyarskaya, Dina;Baratte, Blandine;Josselin, Beatrice;Nedev, Hristo;Bach, Stephane;Iorga, Bogdan I.;Bignon, Jerome;Ruchaud, Sandrine;Al-Mourabit, Ali. And the article was included in Journal of Medicinal Chemistry in 2021.Application In Synthesis of 8-Bromo-3-iodoimidazo[1,2-a]pyridine The following contents are mentioned in the article:
Significant inhibition of Aurora B was achieved by the synthesis of simplified fragments of benzosceptrins and oroidin belonging to the marine pyrrole-2-aminoimidazoles metabolites isolated from sponges. Evaluation of kinase inhibition enabled the discovery of a synthetically accessible rigid acetylenic structural analog EL-228, whose structure could be optimized into the potent CJ2-150. Here we present the synthesis of new inhibitors of Aurora B kinase, which is an important target for cancer therapy through mitosis regulation. The biol. oriented synthesis yielded several nanomolar inhibitors. The optimized compound CJ2-150 showed a non-ATP competitive allosteric mode of action in a mixed-type inhibition for Aurora B kinase. Mol. docking identified a probable binding mode in the allosteric site “F” and highlighted the key interactions with the protein. We describe the improvement of the inhibitory potency and specificity of the novel scaffold as well as the characterization of the mechanism of action. This study involved multiple reactions and reactants, such as 8-Bromo-3-iodoimidazo[1,2-a]pyridine (cas: 1232038-69-5Application In Synthesis of 8-Bromo-3-iodoimidazo[1,2-a]pyridine).
8-Bromo-3-iodoimidazo[1,2-a]pyridine (cas: 1232038-69-5) belongs to iodide derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter.Indole was synthesized in moderate yield via an o-naphthoquinone catalyzed tandem cross-coupling of substituted aniline and benzylamine under aerobic oxidation conditions.Application In Synthesis of 8-Bromo-3-iodoimidazo[1,2-a]pyridine
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com