Venkatesan, Aranapakam M.; Chen, Zecheng; Dos Santos, Osvaldo; Dehnhardt, Christoph; Santos, Efren Delos; Ayral-Kaloustian, Semiramis; Mallon, Robert; Hollander, Irwin; Feldberg, Larry; Lucas, Judy; Yu, Ker; Chaudhary, Inder; Mansour, Tarek S. published the artcile< PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor>, Electric Literature of 20744-39-2, the main research area is substituted triazine derivative preparation PI3K mTOR inhibitor.
A series of mono-morpholino 1,3,5-triazine derivatives bearing a 3-oxa-8-azabicyclo[3.2.1]octane were prepared and evaluated for PI3-kinase/mTOR activity. Replacing one of the bis-morpholines in lead compound I (PKI-587) with 3-oxa-8-azabicyclo[3.2.1]octane and reducing the mol. weight led to compound II (PKI-179), an orally efficacious dual PI3-kinase/mTOR inhibitor. The in vitro activity, in vivo efficacy, and PK properties of II are discussed.
Bioorganic & Medicinal Chemistry Letters published new progress about Enzyme inhibitors. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Electric Literature of 20744-39-2.
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem