| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1362999 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Aranapakam M. Venkatesan, 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,