title: Novel imidazolopyrimidines as dual PI3-Kinase/mTOR inhibitors.
abstract: 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.
authors: Chemical Sciences, Wyeth Research, Pearl River, NY 10965, United States. venkata@wyeth.com
authors: Aranapakam M
authors: AM
authors: Venkatesan
authors: Christoph M
authors: CM
authors: Dehnhardt
authors: Zecheng
authors: Z
authors: Chen
authors: Efren Delos
authors: ED
authors: Santos
authors: Osvaldo
authors: O
authors: Dos Santos
authors: Matthew
authors: M
authors: Bursavich
authors: Adam M
authors: AM
authors: Gilbert
authors: John W
authors: JW
authors: Ellingboe
authors: Semiramis
authors: S
authors: Ayral-Kaloustian
authors: Gulnaz
authors: G
authors: Khafizova
authors: Natasja
authors: N
authors: Brooijmans
authors: Robert
authors: R
authors: Mallon
authors: Irwin
authors: I
authors: Hollander
authors: Larry
authors: L
authors: Feldberg
authors: Judy
authors: J
authors: Lucas
authors: Ker
authors: K
authors: Yu
authors: Jay
authors: J
authors: Gibbons
authors: Robert
authors: R
authors: Abraham
authors: Tarek S
authors: TS
authors: Mansour
mesh_terms: D000255:Adenosine Triphosphate / Q000737:chemistry / Q000378:metabolism; D001665:Binding Sites; D001667:Binding, Competitive; D045744:Cell Line, Tumor; D003198:Computer Simulation; D006801:Humans; D047908:Intracellular Signaling Peptides and Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D019869:Phosphatidylinositol 3-Kinases / Q000378:metabolism; D000081082:Phosphoinositide-3 Kinase Inhibitors; D010766:Phosphorylation; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D051057:Proto-Oncogene Proteins c-akt / Q000378:metabolism; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D058570:TOR Serine-Threonine Kinases
chemical_list: D000255:Adenosine Triphosphate; D047908:Intracellular Signaling Peptides and Proteins; D019869:Phosphatidylinositol 3-Kinases; D000081082:Phosphoinositide-3 Kinase Inhibitors; D047428:Protein Kinase Inhibitors; D017346:Protein Serine-Threonine Kinases; D051057:Proto-Oncogene Proteins c-akt; D011743:Pyrimidines; D058570:TOR Serine-Threonine Kinases; C546842:MTOR protein, human