List of works - Radek Jorda

1,4,6-Trisubstituted imidazo[4,5-c]pyridines as inhibitors of Bruton's tyrosine kinase

scientific article published on 09 December 2020

2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro

scientific article published on 16 April 2015

3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models

scientific article published on 17 April 2019

3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights

scientific article published on 08 October 2019

5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.

scientific article published on 18 January 2016

A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors

scientific article published on 24 July 2013

ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles

scientific article published on 12 January 2017

Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity

scientific article published on 31 August 2019

Anti-leishmanial activity of disubstituted purines and related pyrazolo[4,3-d]pyrimidines

scientific article published on 27 May 2011

Arylazopyrazole AAP1742 inhibits CDKs and induces apoptosis in multiple myeloma cells via Mcl-1 downregulation.

scientific article

Biological Evaluation of Dipyrromethanes in Cancer Cell Lines: Antiproliferative and Pro-apoptotic Properties.

scientific article

CDK9 activity is critical for maintaining MDM4 overexpression in tumor cells

scientific article published on 15 September 2020

Characterization of a Pyrazolo[4,3-d]pyrimidine Inhibitor of Cyclin-Dependent Kinases 2 and 5 and Aurora A With Pro-Apoptotic and Anti-Angiogenic Activity In Vitro

scientific article published on 22 July 2015

Cyclin-dependent kinase inhibitors inspired by roscovitine: purine bioisosteres

scientific article published on January 2012

Degradation of cytokinins by maize cytokinin dehydrogenase is mediated by free radicals generated by enzymatic oxidation of natural benzoxazinones

scientific article published on 14 November 2009

Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations

scientific article published on 19 April 2018

Explicit treatment of active-site waters enhances quantum mechanical/implicit solvent scoring: Inhibition of CDK2 by new pyrazolo[1,5-a]pyrimidines.

scientific article published on 11 December 2016

Exploitation of new structurally diverse d-glucuronamide-containing N-glycosyl compounds: synthesis and anticancer potential

scientific article published on 18 May 2017

Functional p53 in cells contributes to the anticancer effect of the cyclin-dependent kinase inhibitor roscovitine

scientific article published on June 2009

How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?

scientific article published on 05 October 2018

How selective are clinical CDK4/6 inhibitors?

scientific article published on 10 December 2020

New 2,6,9-trisubstituted purine derivatives as Bcr-Abl and Btk inhibitors and as promising agents against leukemia

scientific article published on 17 October 2019

Novel arylazopyrazole inhibitors of cyclin-dependent kinases.

scientific article

Novel inhibitors of cyclin-dependent kinases combat hepatocellular carcinoma without inducing chemoresistance.

scientific article published on 12 August 2013

Novel modified leucine and phenylalanine dipeptides modulate viability and attachment of cancer cells

scientific article published on 07 January 2020

Optimization of norbornyl-based carbocyclic nucleoside analogs as cyclin-dependent kinase 2 inhibitors

scientific article published on 25 March 2020

Pharmacological targeting of CDK9 in cardiac hypertrophy

scientific article published on July 2010

Promising 2,6,9-Trisubstituted Purine Derivatives for Anticancer Compounds: Synthesis, 3D-QSAR, and Preliminary Biological Assays

scientific article published on 25 December 2019

Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity

scientific article

Scaffold hopping of the SYK inhibitor entospletinib leads to broader targeting of the BCR signalosome

scientific article published on 19 July 2020

Selective inhibition reveals cyclin-dependent kinase 2 as another kinase that phosphorylates the androgen receptor at serine 81.

scientific article

Semisynthetic Esters of 17-Hydroxycativic Acid with in Vitro Cytotoxic Activity against Leukemia Cell Lines

scientific article published in January 2017

Structural Basis of the Interaction of Cyclin-Dependent Kinase 2 with Roscovitine and Its Analogues Having Bioisosteric Central Heterocycles.

scientific article published on 27 January 2017

Substituted 2-hydroxy-N-(arylalkyl)benzamides induce apoptosis in cancer cell lines.

scientific article published on 14 August 2013

Synthesis and Evaluation of the Biological Profile of Novel Analogues of Nucleosides and of Potential Mimetics of Sugar Phosphates and Nucleotides

article by Nuno Xavier et al published 9 November 2015 in Synlett

Synthesis and anti-mitotic activity of 2,4- or 2,6-disubstituted- and 2,4,6-trisubstituted-2H-pyrazolo[4,3-c]pyridines.

scientific article published on 16 March 2018

Synthesis and antiproteasomal activity of novel O-benzyl salicylamide-based inhibitors built from leucine and phenylalanine

scientific article published on 15 April 2017

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

scientific article published on 23 June 2012

Synthesis of Novel N9-Substituted Purine Derivatives from Polymer Supported α-Amino Acids.

scientific article published on 25 June 2015

Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines

scientific article published on 18 June 2019

Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors

scientific article published on 19 December 2015

Tetrahydropyrazolo[1,5-a]pyridine-fused steroids and their in vitro biological evaluation in prostate cancer

scientific article published on 30 May 2019

The selective P-TEFb inhibitor CAN508 targets angiogenesis.

scientific article

The synthesis and cholinesterase inhibitory activities of solasodine analogues with seven-membered F ring

scientific article published on 28 October 2020

Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.

scientific article published on 21 October 2017

List of works by Radek Jorda

1,4,6-Trisubstituted imidazo[4,5-c]pyridines as inhibitors of Bruton's tyrosine kinase

2,6,9-Trisubstituted purines as CRK3 kinase inhibitors with antileishmanial activity in vitro

3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models

3-Hydrazinoisatin-based benzenesulfonamides as novel carbonic anhydrase inhibitors endowed with anticancer activity: Synthesis, in vitro biological evaluation and in silico insights

5-Substituted 3-isopropyl-7-[4-(2-pyridyl)benzyl]amino-1(2)H-pyrazolo[4,3-d]pyrimidines with anti-proliferative activity as potent and selective inhibitors of cyclin-dependent kinases.

A novel series of highly potent 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitors

ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles

Activity of 2,6,9-trisubstituted purines as potent PDGFRα kinase inhibitors with antileukaemic activity

Anti-leishmanial activity of disubstituted purines and related pyrazolo[4,3-d]pyrimidines

Arylazopyrazole AAP1742 inhibits CDKs and induces apoptosis in multiple myeloma cells via Mcl-1 downregulation.

Biological Evaluation of Dipyrromethanes in Cancer Cell Lines: Antiproliferative and Pro-apoptotic Properties.

CDK9 activity is critical for maintaining MDM4 overexpression in tumor cells

Characterization of a Pyrazolo[4,3-d]pyrimidine Inhibitor of Cyclin-Dependent Kinases 2 and 5 and Aurora A With Pro-Apoptotic and Anti-Angiogenic Activity In Vitro

Cyclin-dependent kinase inhibitors inspired by roscovitine: purine bioisosteres

Degradation of cytokinins by maize cytokinin dehydrogenase is mediated by free radicals generated by enzymatic oxidation of natural benzoxazinones

Discovery of N2-(4-Amino-cyclohexyl)-9-cyclopentyl- N6-(4-morpholin-4-ylmethyl-phenyl)- 9H-purine-2,6-diamine as a Potent FLT3 Kinase Inhibitor for Acute Myeloid Leukemia with FLT3 Mutations

Explicit treatment of active-site waters enhances quantum mechanical/implicit solvent scoring: Inhibition of CDK2 by new pyrazolo[1,5-a]pyrimidines.

Exploitation of new structurally diverse d-glucuronamide-containing N-glycosyl compounds: synthesis and anticancer potential

Functional p53 in cells contributes to the anticancer effect of the cyclin-dependent kinase inhibitor roscovitine

How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases?

How selective are clinical CDK4/6 inhibitors?

New 2,6,9-trisubstituted purine derivatives as Bcr-Abl and Btk inhibitors and as promising agents against leukemia

Novel arylazopyrazole inhibitors of cyclin-dependent kinases.

Novel inhibitors of cyclin-dependent kinases combat hepatocellular carcinoma without inducing chemoresistance.

Novel modified leucine and phenylalanine dipeptides modulate viability and attachment of cancer cells

Optimization of norbornyl-based carbocyclic nucleoside analogs as cyclin-dependent kinase 2 inhibitors

Pharmacological targeting of CDK9 in cardiac hypertrophy

Promising 2,6,9-Trisubstituted Purine Derivatives for Anticancer Compounds: Synthesis, 3D-QSAR, and Preliminary Biological Assays

Pyrazolo[4,3-d]pyrimidine bioisostere of roscovitine: evaluation of a novel selective inhibitor of cyclin-dependent kinases with antiproliferative activity

Scaffold hopping of the SYK inhibitor entospletinib leads to broader targeting of the BCR signalosome

Selective inhibition reveals cyclin-dependent kinase 2 as another kinase that phosphorylates the androgen receptor at serine 81.

Semisynthetic Esters of 17-Hydroxycativic Acid with in Vitro Cytotoxic Activity against Leukemia Cell Lines

Structural Basis of the Interaction of Cyclin-Dependent Kinase 2 with Roscovitine and Its Analogues Having Bioisosteric Central Heterocycles.

Substituted 2-hydroxy-N-(arylalkyl)benzamides induce apoptosis in cancer cell lines.

Synthesis and Evaluation of the Biological Profile of Novel Analogues of Nucleosides and of Potential Mimetics of Sugar Phosphates and Nucleotides

Synthesis and anti-mitotic activity of 2,4- or 2,6-disubstituted- and 2,4,6-trisubstituted-2H-pyrazolo[4,3-c]pyridines.

Synthesis and antiproteasomal activity of novel O-benzyl salicylamide-based inhibitors built from leucine and phenylalanine

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

Synthesis of Novel N9-Substituted Purine Derivatives from Polymer Supported α-Amino Acids.

Synthesis of novel galeterone derivatives and evaluation of their in vitro activity against prostate cancer cell lines

Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors

Tetrahydropyrazolo[1,5-a]pyridine-fused steroids and their in vitro biological evaluation in prostate cancer

The selective P-TEFb inhibitor CAN508 targets angiogenesis.

The synthesis and cholinesterase inhibitory activities of solasodine analogues with seven-membered F ring

Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.