Structure-activity relationships of phenothiazines and related drugs for inhibition of protein kinase C.

@article{Aftab1991StructureactivityRO,
  title={Structure-activity relationships of phenothiazines and related drugs for inhibition of protein kinase C.},
  author={D T Aftab and Lawrence M. Ballas and Carson R Loomis and William N. Hait},
  journal={Molecular pharmacology},
  year={1991},
  volume={40 5},
  pages={798-805}
}
Phenothiazines are known to inhibit the activity of protein kinase C. To identify structural features that determine inhibitory activity against the enzyme, we utilized a semiautomated assay [Anal. Biochem. 187:84-88 (1990)] to compare the potency of greater than 50 phenothiazines and related compounds. Potency was decreased by trifluoro substitution at position 2 on the phenothiazine nucleus and increased by quinoid structures on the nucleus. An alkyl bridge of at least three carbons… CONTINUE READING