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 …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
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
Small molecular inhibitors of Cyclin dependent kinases (Cdks) are currently being
developed as anticancer therapeutics due to their antiproliferative properties. The purine …
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 …
cyclin-dependent kinases (CDKs), which are established drug targets. Herein, we describe …