Zhu, Gui-Dong; Gong, Jianchun; Claiborne, Akiyo; Woods, Keith W.; Gandhi, Viraj B.; Thomas, Sheela; Luo, Yan; Liu, Xuesong; Shi, Yan; Guan, Ran; Magnone, Shayna R.; Klinghofer, Vered; Johnson, Eric F.; Bouska, Jennifer; Shoemaker, Alexander; Oleksijew, Anatol; Stoll, Vincent S.; De Jong, Ron; Oltersdorf, Tilman; Li, Qun; Rosenberg, Saul H.; Giranda, Vincent L. published the artcile< Isoquinoline-pyridine-based protein kinase B/Akt antagonists: SAR and in vivo antitumor activity>, Synthetic Route of 552331-06-3, the main research area is isoquinoline pyridine derivative preparation Akt kinase inhibitor.
The structure-activity relationships of a series of isoquinoline-pyridine-based protein kinase B/Akt antagonists have been investigated in an effort to improve the major shortcomings of the lead compound (I), including poor pharmacokinetic profiles in several species (e.g., mouse iv t1/2 = 0.3 h, po F = 0%). Chlorination at C-1 position of the isoquinoline improved its pharmacokinetic property in mice (iv t1/2 = 5.0 h, po F = 51%) but resulted in >500-fold drop in potency. In a mouse MiaPaCa-2 xenograft model, an amino analog (II) significantly slowed the tumor growth, however was accompanied by toxicity.
Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 552331-06-3 belongs to class isoquinoline, and the molecular formula is C9H5BrClN, Synthetic Route of 552331-06-3.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem