Potent inhibitors of CDK5 derived from roscovitine: Synthesis, biological evaluation and molecular modelling
L Demange, FN Abdellah, O Lozach, Y Ferandin… - Bioorganic & medicinal …, 2013 - Elsevier
Cyclin dependent kinase 5 (CDK5) is a serine/threonine kinase belonging to the cyclin
dependent kinase (CDK) family. CDK5 is involved in numerous neuronal diseases
(including Alzheimer's or Parkinson's diseases, stroke, traumatic brain injury), pain signaling
and cell migration. In the present Letter, we describe syntheses and biological evaluations of
new 2, 6, 9-trisubstituted purines, structurally related to roscovitine, a promising CDK
inhibitor currently in clinical trials (CDK1/Cyclin B, IC50= 350nM; CDK5/p25, IC50= 200nM) …
dependent kinase (CDK) family. CDK5 is involved in numerous neuronal diseases
(including Alzheimer's or Parkinson's diseases, stroke, traumatic brain injury), pain signaling
and cell migration. In the present Letter, we describe syntheses and biological evaluations of
new 2, 6, 9-trisubstituted purines, structurally related to roscovitine, a promising CDK
inhibitor currently in clinical trials (CDK1/Cyclin B, IC50= 350nM; CDK5/p25, IC50= 200nM) …
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