含有(R)-3-甲基吗啉的三嗪类化合物是哺乳动物雷帕霉素靶蛋白(mTOR)的有效抑制剂，对PI3Kα具有选择性。
Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kalpha.
作者信息
Richard David J, Verheijen Jeroen C, Yu Ker, Zask Arie
机构信息
Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA.
出版信息
Bioorg Med Chem Lett. 2010 Apr 15;20(8):2654-7. doi: 10.1016/j.bmcl.2010.02.029. Epub 2010 Feb 11.
PMID:20223664
Abstract
Potent inhibitors of the mammalian target of rapamycin (mTOR) which contain the triazine scaffold and the (R)-3-methyl morpholine moiety have been identified. Such compounds also demonstrated good selectivity over the related lipid kinase PI3Kalpha. Incorporation of additional functionality at the 4-position of the arylureidophenyl ring resulted in compounds with enhanced cellular activity.
摘要
已鉴定出含有三嗪支架和（R）-3-甲基吗啉部分的雷帕霉素哺乳动物靶标（mTOR）的强效抑制剂。这类化合物对相关脂质激酶PI3Kα也表现出良好的选择性。在芳基脲基苯环的4-位引入额外的官能团，得到了细胞活性增强的化合物。
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