The imidazo[1,2-a]pyridine ring system as a scaffold for potent dual phosphoinositide-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitors was written by Stec, Markian M.;Andrews, Kristin L.;Bo, Yunxin;Caenepeel, Sean;Liao, Hongyu;McCarter, John;Mullady, Erin L.;San Miguel, Tisha;Subramanian, Raju;Tamayo, Nuria;Whittington, Douglas A.;Wang, Ling;Wu, Tian;Zalameda, Leeanne P.;Zhang, Nancy;Hughes, Paul E.;Norman, Mark H.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2015.Related Products of 23707-37-1 This article mentions the following:
Based on lead compound, which was discovered from a high-throughput screen, a series of PI3Kα/mTOR inhibitors were evaluated that contained an imidazo[1,2-a]pyridine as a core replacement for the benzimidazole contained in the lead. By exploring various ring systems that occupy the affinity pocket, two fragments containing a methoxypyridine were identified that gave <100 nM potency toward PI3Kα in enzyme and cellular assays with moderate stability in rat and human liver microsomes. With the two methoxypyridine groups selected to occupy the affinity pocket, analogs were prepared with various fragments intended to occupy the ribose pocket of PI3Kα and mTOR. From these analogs, tertiary alc. I was chosen for in vivo pharmacodynamic evaluation based on its potency in the PI3Kα cellular assay, microsomal stability, and in vivo pharmacokinetic properties. In a mouse liver pharmacodynamic assay, compound I showed 56% inhibition of HFG-induced AKT (Ser473) phosphorylation at a 30 mg/kg dose. In the experiment, the researchers used many compounds, for example, Isoquinolin-7-amine (cas: 23707-37-1Related Products of 23707-37-1).
Isoquinolin-7-amine (cas: 23707-37-1) belongs to isoquinoline derivatives. Isoquinoline is a structural isomer of quinoline, which have antiseptic, antipyretic and anti-cyclic properties, and can be used as antimalarial drugs and for the preparation of other antimalarial medicine. They are also used to make oil-soluble dyes, food colorants, pharmaceuticals, pH indicators and other organic compounds. Related Products of 23707-37-1
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem