In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202.

@article{Raynaud2005InVA,
  title={In vitro and in vivo pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202.},
  author={Florence I. Raynaud and Steven Whittaker and Peter M. Fischer and Steven J. McClue and Michael I. Walton and S. Elaine Barrie and Michelle Dawn Garrett and Paul Rogers and Simon J Clarke and Lloyd R. Kelland and Melanie R. Valenti and Lisa Brunton and Suzanne A. Eccles and D. P. Lane and Paul Workman},
  journal={Clinical cancer research : an official journal of the American Association for Cancer Research},
  year={2005},
  volume={11 13},
  pages={4875-87}
}
PURPOSE To investigate pharmacokinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine, and CYC202 (R-roscovitine; seliciclib) in the HCT116 human colon carcinoma model. EXPERIMENTAL DESIGN The in vitro activity of the agents was determined in a human tumor panel using the sulforhodamine B assay. The concentration and time dependence was established in HCT116 cells. Molecular biomarkers, including RB phosphorylation and… CONTINUE READING