Yu, Tao; Tagat, Jayaram R.; Kerekes, Angela D.; Doll, Ronald J.; Zhang, Yonglian; Xiao, Yushi; Esposite, Sara; Belanger, David B.; Curran, Patrick J.; Mandal, Amit K.; Siddiqui, M. Arshad; Shih, Neng-Yang; Basso, Andrea D.; Liu, Ming; Gray, Kimberly; Tevar, Seema; Jones, Jennifer; Lee, Suining; Liang, Lianzhu; Ponery, Samad; Smith, Elizabeth B.; Hruza, Alan; Voigt, Johannes; Ramanathan, Lata; Prosise, Winifred; Hu, Mengwei published the artcile< Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core>, Product Details of C11H18N2O2, the main research area is imidazopyrazine pyrazolyl isothiazolylamino derivative preparation aurora kinase inhibition activity; pyrazolyl isothiazolylamino imidazopyrazine solubility antitumor activity; Aurora kinase inhibitors; SCH 1473759; aqueous solubility; cell potency; imidazo-[1,2-a]-pyrazine; tumor xenograft model.
The imidazo-[1,2-a]-pyrazine I is a dual inhibitor of Aurora kinases A and B with modest cell potency (IC50 = 250 nM) and low solubility (5 μM). Lead optimization guided by the binding mode led to the acyclic amino alc. II (SCH 1473759), which is a picomolar inhibitor of Aurora kinases (TdF Kd Aur A = 0.02 nM and Aur B = 0.03 nM) with improved cell potency (phos-HH3 inhibition IC50 = 25 nM) and intrinsic aqueous solubility (11.4 mM). It also demonstrated efficacy and target engagement in human tumor xenograft mouse models.
ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 91419-53-3 belongs to class piperidines, and the molecular formula is C11H18N2O2, Product Details of C11H18N2O2.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem