Chemical Sciences, Wyeth Research, Pearl River, NY 10965, United States.
Bioorg Med Chem Lett. 2010 Jan 15;20(2):653-6. doi: 10.1016/j.bmcl.2009.11.057. Epub 2009 Dec 1.
This article describes the syntheses and SAR of a series of imidazolopyrimidine derivatives, which are evaluated as inhibitors of PI3-Kinase (PI3K) and mTOR. These compounds were found to be ATP competitive with good tumor cell growth inhibition, and suppression of pathway specific biomakers such as phosphorylation of Akt at T308.
本文描述了一系列咪唑并嘧啶衍生物的合成和 SAR 研究,这些化合物被评估为 PI3K 抑制剂(PI3K)和 mTOR。这些化合物被发现是 ATP 竞争性的,对肿瘤细胞生长有很好的抑制作用,并抑制了特定途径的生物标志物,如 Akt 在 T308 的磷酸化。