Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer

The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online

Daniel P. Sutherlin; Deepak Sampath; Megan Berry; Georgette Castanedo; Zhigang Chang; Irina Chuckowree; Jenna Dotson; Adrian Folkes; Lori Friedman; Richard Goldsmith; Tim Heffron; Leslie Lee; John Lesnick; Cristina Lewis; Simon Mathieu; Jim Nonomiya; Alan Olivero; Jodie Pang; Wei Wei Prior; Laurent Salphati; Steve Sideris; Qingping Tian; Vickie Tsui; Nan Chi Wan; Shumei Wang; Christian Wiesmann; Susan Wong; Bing-Yan Zhu

2010

Scholarcy highlights

  • The PI3K/AKT/mTOR pathway has been shown to play an important role in cancer. Starting with compounds 1 and 2 as templates,aminopyrimidines were discovered as potent inhibitors of PI3K or both PI3K and mTOR
  • The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online
  • The PI3K/AKT/mTOR pathway has been shown to play an important role in cancer
  • Starting with compounds 1 and 2 as templates,aminopyrimidines were discovered as potent inhibitors of PI3K or both PI3K and mTOR
  • The lead compounds 5 and 21 have good pharmacokinetic parameters, are highly selective, demonstrate knock down of pathway markers in vivo, and are efficacious in xenograft models where the PI3K pathway is deregulated. Both compounds were compared in a PI3Kα mutated MCF7.1 xenograft model and were found to have equivalent efficacy when normalized for exposure

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