| Literature DB >> 20797855 |
Aranapakam M Venkatesan1, Zecheng Chen, Osvaldo dos Santos, Christoph Dehnhardt, Efren Delos Santos, Semiramis Ayral-Kaloustian, Robert Mallon, Irwin Hollander, Larry Feldberg, Judy Lucas, Ker Yu, Inder Chaudhary, Tarek S Mansour.
Abstract
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.Entities:
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Year: 2010 PMID： 20797855 DOI： 10.1016/j.bmcl.2010.07.104
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823