Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy.

@article{Gonzlez2017GenerationOT,
  title={Generation of tricyclic imidazo[1,2-a]pyrazines as novel PI3K inhibitors by application of a conformational restriction strategy.},
  author={S. Mart{\'i}nez Gonz{\'a}lez and Sonsoles Rodr{\'i}guez-Ar{\'i}stegui and Ana-Isabel Hern{\'a}ndez and Carmen Varela and Esther Gonz{\'a}lez Cantalapiedra and R. {\'A}lvarez and Antonio Rodr{\'i}guez Hergueta and J. Bischoff and M. I. Albarr{\'a}n and A. Cebri{\'a} and Elena Cend{\'o}n and D. Cebri{\'a}n and P. Alfonso and J. Pastor},
  journal={Bioorganic \& medicinal chemistry letters},
  year={2017},
  volume={27 11},
  pages={
          2536-2543
        }
}
The involvement of the phosphoinositide 3-kinases (PI3Ks) in several diseases, especially in the oncology area, has singled it as one of the most explored therapeutic targets in the last two decades. Many different inhibitor classes have been developed by the industry and academia with a diverse selectivity profile within the PI3K family. In the present manuscript we report a further exploration of our lead PI3K inhibitor ETP-46321 (Martínez González et al., 2012)1 by the application of a… Expand

References

SHOWING 1-10 OF 22 REFERENCES
Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.
Identification of ETP-46321, a potent and orally bioavailable PI3K α, δ inhibitor.
Rapid identification of ETP-46992, orally bioavailable PI3K inhibitor, selective versus mTOR.
...
1
2
3
...