期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 9, 页码 3426-3435出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm200215y
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A series of inhibitors of mTOR kinase based on a quaternary-substituted dihydrofuropyrimidine was designed and synthesized. The most potent compounds in this series inhibited mTOR kinase with K-i < 1.0 nM and were highly (>100x) selective for mTOR over the closely related PI3 kinases. Compounds in this series showed inhibition of the pathway and antiproliferative activity in cell-based assays. Furthermore, these compounds had excellent mouse PK, and showed a robust PK-PD relationship in a mouse model of cancer.
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