Pyrazolo[4,3-d]pyrimidine Bioisostere of Roscovitine: Evaluation of a Novel Selective Inhibitor of Cyclin-Dependent Kinases with Antiproliferative Activity

R Jorda, L Havlicek, IW McNae… - Journal of medicinal …, 2011 - ACS Publications
Inhibition of cyclin-dependent kinases (CDKs) with small molecules has been suggested as
a strategy for treatment of cancer, based on deregulation of CDKs commonly found in many …

Pyrazolo[1,5-a]-1,3,5-triazine as a Purine Bioisostere: Access to Potent Cyclin-Dependent Kinase Inhibitor (R)-Roscovitine Analogue

F Popowycz, G Fournet, C Schneider… - Journal of medicinal …, 2009 - ACS Publications
Pharmacological inhibitors of cyclin-dependent kinases (CDKs) have a wide therapeutic
potential. Among the CDK inhibitors currently under clinical trials, the 2, 6, 9-trisubstituted …

Molecular docking approach for the design and synthesis of new pyrazolopyrimidine analogs of roscovitine as potential CDK2 inhibitors endowed with pronounced …

OA Hamed, NAE El-Sayed, WR Mahmoud… - Bioorganic …, 2024 - Elsevier
Abstract Cyclin-dependent kinase 2 (CDK2) is a vital protein for controlling cell cycle
progression that is critically associated with various malignancies and its inhibition could …

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 …

Cyclin-dependent kinase inhibitors inspired by roscovitine: purine bioisosteres

R Jorda, K Paruch, V Krystof - Current pharmaceutical design, 2012 - ingentaconnect.com
Roscovitine is a synthetic inhibitor of cyclin-dependent kinases that is currently undergoing
clinical trials as a candidate drug for some oncological indications. Its discovery prompted …

Synthesis, in vitro anticancer activity and in silico studies of certain pyrazole-based derivatives as potential inhibitors of cyclin dependent kinases (CDKs)

EZ Mohammed, WR Mahmoud, RF George… - Bioorganic …, 2021 - Elsevier
New diphenyl-1H-pyrazoles were synthesized and screened for CDK2 inhibition where 8d,
9b, 9c, and 9e exhibited promising activity (IC 50= 51.21, 41.36, 29.31, and 40.54 nM …

Synthesis and in vitro biological evaluation of 2, 6, 9-trisubstituted purines targeting multiple cyclin-dependent kinases

M Zatloukal, R Jorda, T Gucký, E Řezníčková… - European journal of …, 2013 - Elsevier
Several inhibitors of cyclin-dependent kinases (CDKs), including the 2, 6, 9-trisubstituted
purine derivative roscovitine, are currently being evaluated in clinical trials as potential …

8-Azapurines as new inhibitors of cyclin-dependent kinases

L Havlicek, K Fuksova, V Krystof, M Orsag… - Bioorganic & medicinal …, 2005 - Elsevier
Purine inhibitors of cyclin-dependent kinases (CDK) seem to be a potential anticancer drug
candidate as one of the first representatives, roscovitine, is passing Phase II clinical trials for …

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 …

3,5,7-Substituted Pyrazolo[4,3-d]Pyrimidine Inhibitors of Cyclin-Dependent Kinases and Cyclin K Degraders

R Jorda, L Havlicek, M Perina… - Journal of Medicinal …, 2022 - ACS Publications
3, 5, 7-Trisubstituted pyrazolo [4, 3-d] pyrimidines have been identified as potent inhibitors of
cyclin-dependent kinases (CDKs), which are established drug targets. Herein, we describe …