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 …

A review on cyclin-dependent kinase 5: An emerging drug target for neurodegenerative diseases

S Batra, S Jahan, A Ashraf, B Alharby, T Jawaid… - International Journal of …, 2023 - Elsevier
Abstract Cyclin-dependent kinase 5 (CDK5) is the serine/threonine-directed kinase mainly
found in the brain and plays a significant role in developing the central nervous system …

Molecular model of cyclin-dependent kinase 5 complexed with roscovitine

WF de Azevedo Jr, RT Gaspar, F Canduri… - Biochemical and …, 2002 - Elsevier
Here is described a structural model for the binary complex CDK5–roscovitine. Roscovitine
has been shown to potently inhibit cyclin-dependent kinases 1, 2 and 5 (CDK1, 2, and 5) …

Design and synthesis of quinolin-2 (1H)-one derivatives as potent CDK5 inhibitors

W Zhong, H Liu, MR Kaller, C Henley, E Magal… - Bioorganic & medicinal …, 2007 - Elsevier
Cyclin-dependent kinase 5 (CDK5) is a serine/threonine protein kinase and its deregulation
is implicated in a number of neurodegenerative disorders such as Alzheimer's disease …

Mechanism of CDK5/p25 binding by CDK inhibitors

M Mapelli, L Massimiliano, C Crovace… - Journal of medicinal …, 2005 - ACS Publications
The cyclin-dependent kinases (CDK) CDK1, CDK2, CDK4, and CDK6 are serine/threonine
protein kinases targeted in cancer therapy due to their role in cell cycle progression. The …

2, 6, 8, 9-Tetrasubstituted purines as new CDK1 inhibitors

J Moravec, V Kryštof, J Hanuš, L Havlı́ček… - Bioorganic & medicinal …, 2003 - Elsevier
Purine inhibitors of cyclin-dependent kinases attract attention as potential anticancer drugs
because their first representative roscovitine recently entered clinical trials. Although well …

Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1

N Oumata, K Bettayeb, Y Ferandin… - Journal of medicinal …, 2008 - ACS Publications
Cyclin-dependent kinases (CDKs) and casein kinases 1 (CK1) are involved in the two key
molecular features of Alzheimer's disease, production of amyloid-β peptides (extracellular …

Synthesis and evaluation of new potent inhibitors of CK1 and CDK5, two kinases involved in Alzheimer's disease

L Demange, O Lozach, Y Ferandin, NT Hoang… - Medicinal Chemistry …, 2013 - Springer
Abstract Cyclin-dependent kinase 5 (CDK5) and Casein kinase 1 (CK1) are both involved in
the hyperphosphorylation of the Tau protein and in the amyloid-β production, the two major …

Structure–activity relationships of 3, 4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors

RM Rzasa, MR Kaller, G Liu, E Magal… - Bioorganic & medicinal …, 2007 - Elsevier
Cyclin-dependent kinase 5 (CDK5) is a serine/threonine kinase that plays a critical role in
the early development of the nervous system. Deregulation of CDK5 is believed to contribute …

Anti-angiogenic effects of purine inhibitors of cyclin dependent kinases

J Liebl, V Krystof, G Vereb, L Takács, M Strnad… - Angiogenesis, 2011 - Springer
Small molecular inhibitors of Cyclin dependent kinases (Cdks) are currently being
developed as anticancer therapeutics due to their antiproliferative properties. The purine …