Identification of N10-substituted phenoxazines as potent and specific inhibitors of Akt signaling.

@article{Thimmaiah2005IdentificationON,
  title={Identification of N10-substituted phenoxazines as potent and specific inhibitors of Akt signaling.},
  author={Kuntebommanahalli N. Thimmaiah and John Easton and Glen S. Germain and C. Morton and Shantaram Kamath and John K. Buolamwini and Peter James Houghton},
  journal={The Journal of biological chemistry},
  year={2005},
  volume={280 36},
  pages={31924-35}
}
A series of 30 N10-substituted phenoxazines were synthesized and screened as potential inhibitors of Akt. In cellular assays at 5 mum, 17 compounds inhibited insulin-like growth factor 1 (IGF-I)-stimulated phosphorylation of Akt (Ser-473) by at least 50% but did not inhibit IGF-I-stimulated phosphorylation of Erk-1/2 (Thr-202/Tyr-204). Substitutions at the 2-position (Cl or CF3) did not alter inhibitory activity, whereas N10-substitutions with derivatives having acetyl (20B) or morpholino (12B… CONTINUE READING