Imidazo[1,2-a]pyridine-8-carbonitrile(cas: 136117-70-9) belongs to imidazoles.Imidazole rings are also present in imidazole ring alkaloids, which are potential therapeutics for thrombosis, cancer and inflammatory diseases.Quality Control of Imidazo[1,2-a]pyridine-8-carbonitrile Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine.
《Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition》 was written by Reich, Siegfried H.; Sprengeler, Paul A.; Chiang, Gary G.; Appleman, James R.; Chen, Joan; Clarine, Jeff; Eam, Boreth; Ernst, Justin T.; Han, Qing; Goel, Vikas K.; Han, Edward Z. R.; Huang, Vera; Hung, Ivy N. J.; Jemison, Adrianna; Jessen, Katti A.; Molter, Jolene; Murphy, Douglas; Neal, Melissa; Parker, Gregory S.; Shaghafi, Michael; Sperry, Samuel; Staunton, Jocelyn; Stumpf, Craig R.; Thompson, Peggy A.; Tran, Chinh; Webber, Stephen E.; Wegerski, Christopher J.; Zheng, Hong; Webster, Kevin R.. Quality Control of Imidazo[1,2-a]pyridine-8-carbonitrile And the article was included in Journal of Medicinal Chemistry on April 26 ,2018. The article conveys some information:
Dysregulated translation of mRNA plays a major role in tumorigenesis. Mitogen-activated protein kinase interacting kinases (MNK)1/2 are key regulators of mRNA translation integrating signals from oncogenic and immune signaling pathways through phosphorylation of eIF4E and other mRNA binding proteins. Modulation of these key effector proteins regulates mRNA, which controls tumor/stromal cell signaling. Compound 23 (eFT508, 6′-((6-aminopyrimidin-4-yl)amino)-8′-methyl-2’H-spiro-[cyclohexane-1,3′-imidazo[1,5-a]pyridine]-1′,5′-dione hydrochloride), an exquisitely selective, potent dual MNK1/2 inhibitor, was designed to assess the potential for control of oncogene signaling at the level of mRNA translation. The crystal structure-guided design leverages stereoelectronic interactions unique to MNK culminating in a novel pyridone-aminal structure described for the first time in the kinase literature. Compound 23 has potent in vivo antitumor activity in models of diffuse large cell B-cell lymphoma and solid tumors, suggesting that controlling dysregulated translation has real therapeutic potential. Compound 23 is currently being evaluated in Phase 2 clin. trials in solid tumors and lymphoma. Compound 23 is the first highly selective dual MNK inhibitor targeting dysregulated translation being assessed clin. In the experiment, the researchers used many compounds, for example, Imidazo[1,2-a]pyridine-8-carbonitrile(cas: 136117-70-9Quality Control of Imidazo[1,2-a]pyridine-8-carbonitrile)
Imidazo[1,2-a]pyridine-8-carbonitrile(cas: 136117-70-9) belongs to imidazoles.Imidazole rings are also present in imidazole ring alkaloids, which are potential therapeutics for thrombosis, cancer and inflammatory diseases.Quality Control of Imidazo[1,2-a]pyridine-8-carbonitrile Although other azole heterocycles are ubiquitous in a wide range of biologically active natural products, imidazole rings occur predominantly in the natural amino acid histidine.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem