期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 19, 页码 5869-5873出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.07.104
关键词
Phosphatidylinositol-3-kinase (PI3K); PI3K/Akt/mTOR pathway; Dual PI3-kinase/mTOR inhibitors; PKI-587; PKI-179
A series of mono-morpholino 1,3,5-triazine derivatives (8a-8q) bearing a 3-oxa-8-azabicyclo[3.2.1]octane were prepared and evaluated for PI3-kinase/mTOR activity. Replacement of one of the bis-morpholines in lead compound 1 (PKI-587) with 3-oxa-8-azabicyclo[3.2.1] octane and reduction of the molecular weight yielded 8m (PKI-179), an orally efficacious dual PI3-kinase/mTOR inhibitor. The in vitro activity, in vivo efficacy, and PK properties of 8m are discussed. (C) 2010 Published by Elsevier Ltd.
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