新型三环4H-噻唑并[5',4':4,5]吡喃并[2,3-c]吡啶-2-氨基骨架的发现及其在具有高PI3K亚型选择性和强细胞活性的PI3Kα抑制剂中的应用。
Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity.
作者信息
Gerspacher Marc, Fairhurst Robin A, Mah Robert, Roehn-Carnemolla Esther, Furet Pascal, Fritsch Christine, Guthy Daniel A
机构信息
Novartis Institutes for BioMedical Research, Novartis Pharma AG, WKL-136.4.84, CH-4002 Basel, Switzerland.
Novartis Institutes for BioMedical Research, Novartis Pharma AG, WKL-136.4.84, CH-4002 Basel, Switzerland.
出版信息
Bioorg Med Chem Lett. 2015 Sep 1;25(17):3582-4. doi: 10.1016/j.bmcl.2015.06.077. Epub 2015 Jun 30.
A novel, previously undescribed 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine tricyclic scaffold has been discovered. The application of this novel chemotype leading to a potent and selective prototype PI3Kα inhibitor with favorable physicochemical and PK-properties is described.
已发现一种新型的、此前未描述过的4H-噻唑并[5',4':4,5]吡喃并[2,3-c]吡啶三环骨架。本文描述了这种新型化学类型的应用，该应用产生了一种具有良好物理化学性质和药代动力学性质的强效且选择性的PI3Kα抑制剂原型。
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