Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.

@article{Certal2014DiscoveryAO,
  title={Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers.},
  author={Victor F Certal and Jean-Christophe Carry and Frank Halley and Angela Virone-Oddos and Fabienne Thompson and Bruno Filoche-Romm{\'e} and Youssef El-Ahmad and Andreas Karlsson and V{\'e}ronique Charrier and C{\'e}cile Delorme and Alexey Rak and P. Y. Abecassis and C{\'e}line Amara and Lo{\"i}c Vincent and H{\'e}l{\`e}ne Bonnevaux and J. Nicol{\'a}s and Magali Mathieu and Thomas Bertrand and Jean-Pierre Marquette and Nadine Michot and Tsiala B{\'e}nard and Marc-Antoine Perrin and Olivier Lemaitre and St{\'e}phane Guerif and S{\'e}bastien Gauthier Perron and Sylvie Monget and florence gruss-leleu and Gilles Doerflinger and Houlfa Guizani and Maurice Brollo and Laurence Delbarre and Luc Bertin and Patrick Richepin and V{\'e}ronique Loyau and Carlos Garc{\'i}a-echeverr{\'i}a and Christoph Lengauer and Laurent Schio},
  journal={Journal of medicinal chemistry},
  year={2014},
  volume={57 3},
  pages={
          903-20
        }
}
Compelling molecular biology publications have reported the implication of phosphoinositide kinase PI3Kβ in PTEN-deficient cell line growth and proliferation. These findings supported a scientific rationale for the development of PI3Kβ-specific inhibitors for the treatment of PTEN-deficient cancers. This paper describes the discovery of 2-[2-(2,3-dihydro-indol-1-yl)-2-oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one (7) and the optimization of this new series of active and selective pyrimidone… CONTINUE READING
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Inhibiting PI3Kβ with AZD8186 Regulates Key Metabolic Pathways in PTEN-Null Tumors.

  • Clinical cancer research : an official journal of the American Association for Cancer Research
  • 2017

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