… describe syntheses and biological evaluations of new 2,6,9-trisubstituted purines, structurally
related to roscovitine, a promising CDK inhibitor currently in … = 350 nM; CDK5/p25, IC 50 …

… In addition, they are inhibit CDK5 enzyme using roscovitine as a … Molecular modelling and
docking study … Å, the previous theoretical results obtained from molecular docking proved the …

… potent inhibitors of the CDK1 and CDK5 kinases. We thus developed an efficient and modular
synthetic … Our interest in the synthesis of kinase inhibitors comes from the screening of the …

… Indirubin-3‘-oxime is also a potent inhibitor of CDK5/p25 (IC 50 … In particular, we have obtained
a very well diffracting crystal … CDK5/p25 complex with (R)-roscovitine. Besides providing a …

… of CDK5 in early 1990s, a lot of progress has been made in … major goals of designing selective
CDK5/p25 inhibitors targeting … Even though R- roscovitine (2.1) had been explored as one …

… Roscovitine derivatives are potent inhibitors of cyclin-dependent kinase 5 (… that the
conformation of CDK5/R-roscovitine obtained from current MD simulation is reliable. Although there …

… derived from the olomoucine/roscovitine lead structure were … and (R)-roscovitine, all the
CDK1 and CDK5 inhibitors (9–24) … potent inhibitor of CDK5) and compound 15 (6 times more …

… find selective cyclin-dependent kinase inhibitors (Cdki) have been made during the last 15
years. … Roscovitine is a potent inhibitor of Cdk5 which has important function in the developing …

… derived cell line MCF7. The most active derivative 16g possessed an identical side chain in
the C2 position to roscovitine… towards protein kinases compared to roscovitine. Nevertheless, …

… SF-539 cell line were obtained with the best results, using Roscovitine as a positive control.
… , but also inhibits CDK5, that is involved in cell migration. This dual effect make Roscovitine a …