Synthesis and in vitro evaluation of novel 2,6,9-trisubstituted purines acting as cyclin-dependent kinase inhibitors.

@article{Legraverend1999SynthesisAI,
  title={Synthesis and in vitro evaluation of novel 2,6,9-trisubstituted purines acting as cyclin-dependent kinase inhibitors.},
  author={Michel Legraverend and Otto Ludwig and Emile Bisagni and Sophie Leclerc and Laurent Meijer and Nicole Giocanti and Ramin Sadri and Vincent Favaudon},
  journal={Bioorganic & medicinal chemistry},
  year={1999},
  volume={7 7},
  pages={
          1281-93
        }
}
Novel C-2, C-6, N-9 trisubstituted purines derived from the olomoucine/roscovitine lead structure were synthesized and evaluated for their ability to inhibit starfish oocyte CDK1/cyclin B, neuronal CDK5/p35 and erk1 kinases in purified extracts. Structure activity relationship studies showed that increased steric bulk at N-9 reduces the inhibitory potential whereas substitution of the aminoethanol C-2 side chain by various groups of different size (methyl, propyl, butyl, phenyl, benzyl) only… CONTINUE READING

Citations

Publications citing this paper.
SHOWING 1-10 OF 11 CITATIONS

8-Amino-adenosine inhibits multiple mechanisms of transcription.

  • Molecular cancer therapeutics
  • 2010
VIEW 1 EXCERPT
CITES BACKGROUND

References

Publications referenced by this paper.