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List of works by Stefan Laufer

1,4-Dimethyl-2-phenyl-6,7-dihydro-1H-pyrazolo-[4,3-b]pyridine-3,5(2H,4H)-dione.

scientific article published on 14 September 2011

1-[2-(Benzylamino)-4-pyridyl]-2-(4-fluorophenyl)ethane-1,2-dione

scientific article published on May 29, 2009

2-(3,4,5-Trimethoxy-phen-yl)-1H-pyrrolo[2,3-b]pyridine.

scientific article published on 14 November 2009

2-(4-Fluoro-phen-yl)-3-(4-pyrid-yl)pyrido[2,3-b]pyrazine.

scientific article published on 26 September 2009

2-(Bicyclo-[2.2.1]hept-5-en-2-yl)-1H-pyrrolo-[2,3-b]pyridine

scientific article published on 26 June 2010

2-[(1-Methyl-1H-pyrrol-2-yl)carbonyl-meth-yl]isoindoline-1,3-dione.

scientific article published on 9 September 2009

3,4-Diaryl-isoxazoles and -imidazoles as potent dual inhibitors of p38alpha mitogen activated protein kinase and casein kinase 1delta.

scientific article

3-(2,4-Difluoroanilino)-9-nitrodibenzo[b,e]oxepin-11(6H)-one

scientific article published on February 2, 2011

3-(2,4-Dimeth-oxy-anilino)-8-meth-oxy-dibenz[b,e]oxepin-11(6H)-one.

scientific article published on 26 January 2011

3-(2-Fluoro-phen-yl)-6-(phenoxy-meth-yl)-1,2,4-triazolo[3,4-b][1,3,4]thia-diazole.

scientific article published on 12 March 2008

3-(4-Fluoro-phen-yl)-2-(4-pyrid-yl)pyrido[2,3-b]pyrazine.

scientific article published on 26 September 2009

3-(4-Fluorophenyl)-6-methoxy-2-(4-pyridyl)quinoxaline

scientific article published on June 20, 2009

4-(4-Fluoro-phen-yl)-1-methoxy-methyl-2-phenyl-1H-imidazole

scientific article published on 23 October 2009

4-(4-Fluorophenyl)-2-methyl-3-(1-oxy-4-pyridyl)isoxazol-5(2H)-one

scientific article published on January 23, 2008

4-Chloro-1-(4-methyl-phenyl-sulfon-yl)-1H-pyrrolo[2,3-b]pyridine.

scientific article published on 7 November 2009

4-Chloro-7-methoxy-methyl-2-phenyl-7H-pyrrolo[2,3-b]pyridine

scientific article published on 13 March 2010

4-[2-(4-Fluoro-phen-yl)-1H-pyrrol-3-yl]pyridine

scientific article

4-[2-(4-Fluoro-phen-yl)furan-3-yl]pyridine

scientific article published on 4 February 2009

4-[3-(4-Fluorophenyl)quinoxalin-2-yl]-N-isopropylpyridin-2-amine

scientific article published on May 20, 2009

4-[4-(4-Fluoro-phen-yl)-2-methyl-5-oxo-2,5-dihydro-isoxazol-3-yl]-1-methyl-pyridinium iodide-4-[3-(4-fluoro-phen-yl)-2-methyl-5-oxo-2,5-dihydro-isoxazol-4-yl]-1-methyl-pyridinium iodide (0.6/0.4).

scientific article published on 18 December 2007

4-[5-(4-Fluoro-phen-yl)-1H-imidazol-4-yl]pyridine.

scientific article published on 21 February 2009

5-(4-Fluoro-phen-yl)-4-(4-pyrid-yl)-1,3-oxazol-2-amine.

scientific article published on 24 March 2010

6-(4-Chloro-phen-yl)-7-phenyl-2,3-dihydro-1H-pyrrolizine-5-carbaldehyde

scientific article published on 11 August 2011

6-(4-Meth-oxy-phen-yl)-7-phenyl-2,3-dihydro-1H-pyrrolizine-5-carbaldehyde

scientific article published on 27 August 2011

6-Amino-1-benzyl-4-(4-chlorophenyl)-3-(4-pyridyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile

scientific article published on March 12, 2008

7-[4-(4-Fluoro-phen-yl)-2-methyl-sulfanyl-1H-imidazol-5-yl]tetra-zolo[1,5-a]pyridine.

scientific article published on 27 January 2010

A Diverse and Versatile Regiospecific Synthesis of Tetrasubstituted Alkylsulfanylimidazoles as p38α Mitogen-Activated Protein Kinase Inhibitors

scientific article

A MYC-aurora kinase A protein complex represents an actionable drug target in p53-altered liver cancer

scientific article published on 23 May 2016

A Multicomponent Carba-Betti Strategy to Alkylidene Heterodimers - Total Synthesis and Structure-Activity Relationships of Arzanol

A direct ELISA assay for quantitative determination of the inhibitory potency of small molecules inhibitors for JNK3

scientific article published on January 22, 2011

A fraction of stem bark extract of Entada africana suppresses lipopolysaccharide-induced inflammation in RAW 264.7 cells

scientific article published on 21 June 2013

A frozen analogue approach to aminopyridinylimidazoles leading to novel and promising p38 MAP kinase inhibitors

article by Roland Selig et al published 20 September 2012 in Journal of Medicinal Chemistry

A new in vitro model to study cellular responses after thermomechanical damage in monolayer cultures

scientific article

A p38 substrate-specific MK2-EGFP translocation assay for identification and validation of new p38 inhibitors in living cells: a comprising alternative for acquisition of cellular p38 inhibition data

scientific article

ACKR3 regulates platelet activation and ischemia-reperfusion tissue injury

scientific article published on 05 April 2022

Abietane diterpenes induce cytotoxic effects in human pancreatic cancer cell line MIA PaCa-2 through different modes of action

scientific article published on March 19, 2012

Accelerated clearance of Plasmodium-infected erythrocytes in sickle cell trait and annexin-A7 deficiency.

scientific article published on 4 November 2009

Achiral-chiral LC/LC-MS/MS coupling for determination of chiral discrimination effects in phenprocoumon metabolism.

scientific article published in April 2005

An immunosorbent, nonradioactive p38 MAP kinase assay comparable to standard radioactive liquid-phase assays

scientific article published in September 2005

An in-vitro screening assay for the detection of inhibitors of proinflammatory cytokine synthesis: a useful tool for the development of new antiarthritic and disease modifying drugs.

scientific article published in December 2002

An optimized and versatile synthesis to pyridinylimidazole-type p38α mitogen activated protein kinase inhibitors

scientific article published on 9 September 2015

Anti-inflammatory activity of myricetin-3-O-beta-D-glucuronide and related compounds

scientific article published on 01 November 1998

Anti-inflammatory drugs: new multitarget compounds to face an old problem. The dual inhibition concept.

scientific article published in May 2001

Antinociceptive, anti-inflammatory and gastroprotective effects of a hydroalcoholic extract from the leaves of Eugenia punicifolia (Kunth) DC. in rodents.

scientific article published on 13 October 2014

Antioxidative properties of the gastrointestinal phytopharmaceutical remedy STW 5 (Iberogast)

scientific article published on 18 May 2006

Antithrombotic and platelet function inhibiting effects of ML3000, a new antiinflammatory drug with Cox/5-LOX inhibitory activity

scientific article (publication date: March 2002)

Arachidonoyl-phosphatidylcholine oscillates during the cell cycle and counteracts proliferation by suppressing Akt membrane binding

scientific article published on January 28, 2013

Are peptides a solution for the treatment of hyperactivated JAK3 pathways?

scientific article published on 30 March 2019

Are vanadium compounds drugable? Structures and effects of antidiabetic vanadium compounds: a critical review.

scientific article

Arylpyrrolizines as inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1) or as dual inhibitors of mPGES-1 and 5-lipoxygenase (5-LOX)

scientific article published on 01 August 2009

Assessing the Target Differentiation Potential of Imidazole-Based Protein Kinase Inhibitors

scientific article published on December 11, 2012

Aza-analogue dibenzepinone scaffolds as p38 mitogen-activated protein kinase inhibitors: design, synthesis, and biological data of inhibitors with improved physicochemical properties

scientific article

Bioinformatical evaluation of modified nucleosides as biomedical markers in diagnosis of breast cancer

scientific article published on 01 May 2008

Biological Evaluation and Structural Determinants of p38α Mitogen‐Activated‐Protein Kinase and c‐Jun‐N‐Terminal Kinase 3 Inhibition by Flavonoids

scientific article published on December 10, 2010

Biological studies on Brazilian plants used in wound healing.

scientific article

COX-3--a virtual pain target in humans?

scientific article published in December 2003

Catechin derivatives from Parapiptadenia rigida with in vitro wound-healing properties.

scientific article

Chemical Space Exploration of Oxetanes

scientific article published on 02 November 2020

Chiral sulfoxides as metabolites of 2-thioimidazole-based p38α mitogen-activated protein kinase inhibitors: enantioselective synthesis and biological evaluation.

scientific article published on 12 April 2011

Click Chemistry: Novel Applications in Cell Biology and Drug Discovery.

scientific article published on 25 October 2017

Colocalization of the VEGF-R2 and the common IL-3/GM-CSF receptor beta chain to lipid rafts leads to enhanced p38 activation.

scientific article

Correction to Tetra-substituted pyridinylimidazoles as dual inhibitors of p38α mitogen-activated protein kinase and c-Jun N-terminal kinase 3 for potential treatment of neurodegenerative diseases.

scientific article

Decisive role of water and protein dynamics in residence time of p38α MAP kinase inhibitors

scientific article published on 28 January 2022

Deoxyhypusine hydroxylase from Plasmodium vivax, the neglected human malaria parasite: molecular cloning, expression and specific inhibition by the 5-LOX inhibitor zileuton

scientific article

Design and synthesis of novel fluorescently labeled analogs of vemurafenib targeting MKK4

scientific article published on 04 October 2020

Design and synthesis of tricyclic JAK3 inhibitors with picomolar affinities as novel molecular probes

scientific article published on 8 January 2014

Design, Synthesis and Biological Evaluation of 7-Chloro-9H-pyrimido[4,5-b]indole-based Glycogen Synthase Kinase-3β Inhibitors

scientific article published on 25 June 2019

Design, Synthesis, and Biological Evaluation of Novel Disubstituted Dibenzosuberones as Highly Potent and Selective Inhibitors of p38 Mitogen Activated Protein Kinase

scientific article published on June 15, 2012

Design, Synthesis, and Biological Evaluation of Novel Type I1/2 p38α MAP Kinase Inhibitors with Excellent Selectivity, High Potency, and Prolonged Target Residence Time by Interfering with the R-Spine.

scientific article published on 23 August 2017

Design, synthesis and SAR of phenylamino-substituted 5,11-dihydro-dibenzo[a,d]cyclohepten-10-ones and 11H-dibenzo[b,f]oxepin-10-ones as p38 MAP kinase inhibitors.

scientific article published in April 2010

Design, synthesis and characterization of N9/N7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors

scientific article published on 30 April 2008

Design, synthesis and structure-activity relationship of functionalized tetrahydro-β-carboline derivatives as novel PDE5 inhibitors.

scientific article published on 22 December 2010

Design, synthesis, and biological evaluation of phenylamino-substituted 6,11-dihydro-dibenzo[b,e]oxepin-11-ones and dibenzo[a,d]cycloheptan-5-ones: novel p38 MAP kinase inhibitors

scientific article published on 01 December 2006

Determination of the wound healing effect of Calendula extracts using the scratch assay with 3T3 fibroblasts.

scientific article published on 23 September 2009

Development and optimization of a non-radioactive JNK3 assay

scientific article published on 01 September 2006

Development of a microsphere-based p38alpha MAP kinase no-wash assay.

scientific article published on 7 June 2006

Development of a p38δ mitogen activated protein kinase ELISA assay for the quantitative determination of inhibitor activity

scientific article published on March 15, 2012

Development of an in-vitro test system for the evaluation of cyclooxygenase-2 inhibitors

scientific article published on 01 March 1999

Development of first lead structures for phosphoinositide 3-kinase-C2γ inhibitors.

scientific article

Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold

scientific article published on 13 June 2018

Dibenzosuberones as p38 Mitogen-Activated Protein Kinase Inhibitors with Low ATP Competitiveness and Outstanding Whole Blood Activity

scientific article published on December 27, 2012

Different methods for testing potential cyclooxygenase-1 and cyclooxygenase-2 inhibitors.

scientific article published on January 2010

Differentiation of cardiomyocytes and generation of human engineered heart tissue

scientific article published on 11 May 2017

Discovery and Evaluation of Enantiopure 9H-pyrimido[4,5-b]indoles as Nanomolar GSK-3β Inhibitors with Improved Metabolic Stability

scientific article published on 22 October 2020

Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38α MAPK/PDE-4 Inhibitor with Activity against TNFα-Related Diseases

scientific article published on 14 June 2017

Discovery of a Novel Class of Covalent Dual Inhibitors Targeting the Protein Kinases BMX and BTK

scientific article published on 04 December 2020

Discovery of a novel series of tetrahydro-β-carbolines inducing autophagic cell death in human metastatic melanoma.

scientific article published on 20 March 2014

Discovery of novel orally active anti-inflammatory N-phenylpyrazolyl-N-glycinyl-hydrazone derivatives that inhibit TNF-α production

scientific article

Donated chemical probes for open science

scientific article published on 20 April 2018

Drug Discovery: A Modern Decathlon

scientific article published on 06 March 2013

Dynamics in the p38alpha MAP kinase-SB203580 complex observed by liquid-state NMR spectroscopy

scientific article published on 01 January 2008

Effect of TGFβ on Na+/K+ ATPase activity in megakaryocytes.

scientific article published on 27 August 2014

Effect of TGFβ on calcium signaling in megakaryocytes.

scientific article

Efficacy and gastrointestinal tolerability of ML3403, a selective inhibitor of p38 MAP kinase and CBS-3595, a dual inhibitor of p38 MAP kinase and phosphodiesterase 4 in CFA-induced arthritis in rats

scientific article published on 15 November 2013

Emerging and Re-Emerging Warheads for Targeted Covalent Inhibitors: Applications in Medicinal Chemistry and Chemical Biology

scientific article published on 25 January 2019

Entada africana fraction CH₂Cl₂/MEOH 5% inhibits inducible nitric oxide synthase and pro-inflammatory cytokines gene expression induced by lipopolysaccharide in microglia

scientific article

Extract from gum resin of Boswellia serrata decreases IA(2)-antibody in a patient with "Late onset Autoimmune Diabetes of the Adult" (LADA)

scientific article published on 31 March 2014

Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors

scientific article published on 26 November 2019

Fighting cancer drug resistance: Opportunities and challenges for mutation-specific EGFR inhibitors.

scientific article published on 12 May 2015

Fine-tuned PEGylation of chitosan to maintain optimal siRNA-nanoplex bioactivity.

scientific article published on 08 January 2016

Flavonoids Inhibit COX-1 and COX-2 Enzymes and Cytokine/Chemokine Production in Human Whole Blood

article

Fluorescence polarization binding assay to develop inhibitors of inactive p38alpha mitogen-activated protein kinase.

scientific article published on 20 February 2010

Four new flavonol glycosides from the leaves of Brugmansia suaveolens

scientific article published on 22 May 2014

From 2-Alkylsulfanylimidazoles to 2-Alkylimidazoles: An Approach towards Metabolically More Stable p38α MAP Kinase Inhibitors.

scientific article published on 14 October 2017

From five- to six-membered rings: 3,4-diarylquinolinone as lead for novel p38MAP kinase inhibitors

scientific article published on 27 February 2007

From off-to on-target: New BRAF-inhibitor-template-derived compounds selectively targeting mitogen activated protein kinase kinase 4 (MKK4)

scientific article published on 24 October 2020

Fucoxanthin Induced Suicidal Death of Human Erythrocytes

scientific article published on 14 December 2015

High anti-inflammatory activity of harpagoside-enriched extracts obtained from solvent-modified super- and subcritical carbon dioxide extractions of the roots of Harpagophytum procumbens.

scientific article published in January 2006

IL-1β, IL-18, and eicosanoids promote neutrophil recruitment to pore-induced intracellular traps following pyroptosis.

scientific article published on 28 September 2016

Identification of new γ-hydroxybutenolides that preferentially inhibit the activity of mPGES-1.

scientific article

Identification of regioisomers in a series of N-substituted pyridin-4-yl imidazole derivatives by regiospecific synthesis, GC/MS, and 1H NMR.

scientific article published in May 2003

Identification of urinary modified nucleosides and ribosylated metabolites in humans via combined ESI-FTICR MS and ESI-IT MS analysis.

scientific article published on 28 June 2008

Imidazole inhibitors of cytokine release: probing substituents in the 2 position.

scientific article published in October 2002

Implications for selectivity of 3,4-diarylquinolinones as p38alphaMAP kinase inhibitors

scientific article

In Vivo Hypoxia PET Imaging Quantifies the Severity of Arthritic Joint Inflammation in Line with Overexpression of Hypoxia-Inducible Factor and Enhanced Reactive Oxygen Species Generation

scientific article published on 9 February 2017

In vitro cytotoxic activity of abietane diterpenes from Peltodon longipes as well as Salvia miltiorrhiza and Salvia sahendica.

scientific article

In vivo RNAi screening identifies a mechanism of sorafenib resistance in liver cancer.

scientific article

Induction but not inhibition of COX-2 confers human lung cancer cell apoptosis by celecoxib.

scientific article published on 12 August 2013

Inferential NMR/X-ray-based structure determination of a dibenzo[a,d]cycloheptenone inhibitor-p38α MAP kinase complex in solution

scientific article

Influence of annexin A7 on insulin sensitivity of cellular glucose uptake

scientific article published on 07 June 2014

Influence of p38MAPK inhibition on IL-1beta-stimulated human chondrocytes: a microarray approach.

scientific article published in May 2009

Influence of willow bark extract on cyclooxygenase activity and on tumor necrosis factor alpha or interleukin 1 beta release in vitro and ex vivo

scientific article published in March 2003

Inhibition of GSK3 differentially modulates NF-kappaB, CREB, AP-1 and beta-catenin signaling in hepatocytes, but fails to promote TNF-alpha-induced apoptosis

scientific article published on 31 December 2007

Inhibitors of c-Jun N-terminal kinases: an update.

scientific article

Interference of boswellic acids with the ligand binding domain of the glucocorticoid receptor

scientific article published on 20 February 2014

Investigations of SCIO-469-like compounds for the inhibition of p38 MAP kinase.

scientific article published on 14 January 2009

Isoxazolone based inhibitors of p38 MAP kinases.

scientific article published on 29 March 2008

Licofelone, a dual COX/5-LOX inhibitor, induces apoptosis in HCA-7 colon cancer cells through the mitochondrial pathway independently from its ability to affect the arachidonic acid cascade

scientific article published on 21 November 2007

Lung Cancer: EGFR Inhibitors with Low Nanomolar Activity against a Therapy-Resistant L858R/T790M/C797S Mutant.

scientific article

Mechanistic role of p38 MAPK in gastric cancer dissemination in a rodent model peritoneal metastasis.

scientific article

Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood

scientific article

Metabonomics in cancer diagnosis: mass spectrometry-based profiling of urinary nucleosides from breast cancer patients

scientific article published on 01 June 2008

Methyl 4-[5-(4-fluoro-phen-yl)-4-(pyridin-4-yl)-1H-imidazol-2-ylsulfan-yl]butanoate

scientific article published on 7 June 2008

Modeling and benchmark data set for the inhibition of c-Jun N-terminal kinase-3.

scientific article

Modified acidic nonsteroidal anti-inflammatory drugs as dual inhibitors of mPGES-1 and 5-LOX.

scientific article

N-(4-Chloro-pyridin-2-yl)-N-meth-oxy-methyl-4-methyl-benzene-sulfonamide

scientific article published on 27 November 2010

N-[3-(5-Oxo-10,11-dihydro-5H-dibenzo[a,d]cyclo-hepten-2-ylamino)phen-yl]furan-3-carboxamide.

scientific article published on 17 April 2010

N-{2-Methyl-5-[(5-oxo-10,11-dihydro-5H-dibenzo[a,d]cyclo-hepten-2-yl)amino]-phen-yl}benzamide.

scientific article published on 30 June 2010

N-{4-[3-(4-Fluorophenyl)pyrido[2,3-b]pyrazin-2-yl]-2-pyridyl}isopropylamine

scientific article published on September 26, 2009

N-{4-[4-(4-Fluoro-phen-yl)-1-methyl-2-[(R)-methyl-sulfin-yl]-1H-imidazol-5-yl]-2-pyridyl}acetamide dihydrate.

scientific article published on 12 December 2009

N-{4-[4-(4-Fluorophenyl)-1-(2-methoxyethyl)-2-methylsulfanyl-1H-imidazol-5-yl]-2-pyridyl}-2-methyl-3-phenylpropionamide

scientific article published on November 21, 2009

Neuromodulatory effects of Calyptranthes grandifolia extracts against 6-hydroxydopamine-induced neurotoxicity in SH-SY5Y cells.

scientific article published on 23 September 2016

Neuroprotective potential of Myrciaria plinioides D. Legrand extract in an in vitro human neuroblastoma model

scientific article published on 15 October 2019

New Frontiers in Kinases: Second Generation Inhibitors-Going beyond Cancer.

scientific article published on 8 January 2015

New Horizons in Drug Discovery - Understanding and Advancing Kinase Inhibitors

scientific article published on 15 July 2020

New approaches to the treatment of inflammatory disorders small molecule inhibitors of p38 MAP kinase.

scientific article

New insights into novel inhibitors against deoxyhypusine hydroxylase from plasmodium falciparum: compounds with an iron chelating potential

scientific article published on 26 February 2015

Novel 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors.

scientific article published on 31 October 2013

Novel hinge-binding motifs for Janus kinase 3 inhibitors: a comprehensive structure-activity relationship study on tofacitinib bioisosteres.

scientific article

One-pot synthesis of 4,6-diaryl-2-oxo(imino)-1,2-dihydropyridine-3-carbonitrile; a New Scaffold for p38alpha MAP kinase inhibition

scientific article

Optimized Target Residence Time: Type I1/2 Inhibitors for p38α MAP Kinase with Improved Binding Kinetics through Direct Interaction with the R-Spine.

scientific article published on 11 April 2017

Osteoarthritis therapy--are there still unmet needs?

scientific article published on February 2004

P38 Kinase, SGK1 and NF-κB Dependent Up-Regulation of Na+/Ca2+ Exchanger Expression and Activity Following TGFß1 Treatment of Megakaryocytes.

scientific article published on 15 August 2017

PGE(2) in the regulation of programmed erythrocyte death

scientific article (publication date: May 2005)

Pharmacokinetics of ML3403 ({4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-amine), a 4-Pyridinylimidazole-type p38 mitogen-activated protein kinase inhibitor.

scientific article published on 7 March 2007

Prediction of breast cancer by profiling of urinary RNA metabolites using Support Vector Machine-based feature selection.

scientific article published on 05 April 2009

Profile and Molecular Modeling of 3-(Indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole-2,5dione (1) as a Highly Selective VEGF-R2/3 Inhibitor

article published in 2006

Progress towards a public chemogenomic set for protein kinases and a call for contributions

scientific article

Promiscuity analysis of a kinase panel screen with designated p38 alpha inhibitors

scientific article published on 20 December 2019

Proteasome Activation by Small Molecules.

scientific article

Protective effects of licofelone, a 5-lipoxygenase and cyclo-oxygenase inhibitor, versus naproxen on cartilage loss in knee osteoarthritis: a first multicentre clinical trial using quantitative MRI.

scientific article

Pyridinylimidazoles as dual glycogen synthase kinase 3β/p38α mitogen-activated protein kinase inhibitors

scientific article published on 24 April 2019

Pyridinylquinoxalines and pyridinylpyridopyrazines as lead compounds for novel p38 alpha mitogen-activated protein kinase inhibitors.

scientific article published in February 2010

Quantitative determination of piritramide in human plasma and urine by off- and on-line solid-phase extraction liquid chromatography coupled to tandem mass spectrometry.

scientific article

Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting

scientific article published on 29 July 2017

Regioisomeric 5(3)-aminomethyl-3(5)-phenylisoxazoles: synthesis, spectroscopic discrimination, and muscarinic activity

scientific article published on 01 May 1995

Regulation of coronary venular barrier function by blood borne inflammatory mediators and pharmacological tools: insights from novel microvascular wall models

scientific article published on 11 November 2011

Review of Trials Currently Testing Stem Cells for Treatment of Respiratory Diseases: Facts Known to Date and Possible Applications to COVID-19

scientific article published on 22 August 2020

SCISSOR-Spinal Cord Injury Study on Small molecule-derived Rho inhibition: a clinical study protocol

scientific article published on 26 July 2016

Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket

scientific article published on 7 November 2016

Sesquiterpene lactones as inhibitors of IL-8 expression in HeLa cells.

scientific article

Skepinone-L is a selective p38 mitogen-activated protein kinase inhibitor

scientific article published on December 25, 2011

Skepinone-L, a novel potent and highly selective inhibitor of p38 MAP kinase, effectively impairs platelet activation and thrombus formation.

scientific article

Small molecular anti-cytokine agents.

scientific article

Small-molecule-induced Rho-inhibition: NSAIDs after spinal cord injury

scientific article

Solution-phase parallel synthesis of ruxolitinib-derived Janus kinase inhibitors via copper-catalyzed azide-alkyne cycloaddition.

scientific article

Special Issue: Kinase inhibitors

scientific article published on 22 July 2018

Spinal inhibition of p38 MAP kinase reduces inflammatory and neuropathic pain in male but not female mice: Sex-dependent microglial signaling in the spinal cord

scientific article

Stimulating Effect of Sclareol on Suicidal Death of Human Erythrocytes.

scientific article published on 11 July 2016

Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors

scientific article published on 03 April 2020

Structural and conformational analysis of proanthocyanidins from Parapiptadenia rigida and their wound-healing properties

scientific article published on 10 May 2011

Structural approaches to explain the selectivity of COX-2 inhibitors: is there a common pharmacophore?

scientific article

Substituted isoxazoles as potent inhibitors of p38 MAP kinase

scientific article published on 01 February 2006

Successful structure-based design of recent p38 MAP kinase inhibitors.

scientific article published on January 2009

Synthesis and biological testing of N-aminoimidazole-based p38alpha MAP kinase inhibitors.

scientific article published in July 2010

Synthesis and biological testing of purine derivatives as potential ATP-competitive kinase inhibitors.

scientific article published in February 2005

Synthesis and structure‑activity‑relationship of 3,4‑Diaryl‑1H‑pyrrolo[2,3‑b]pyridines as irreversible Inhibitors of mutant EGFR‑L858R/T790M

scientific article published on 22 November 2018

Synthesis, biological testing, and binding mode prediction of 6,9-diarylpurin-8-ones as p38 MAP kinase inhibitors

scientific article published on 06 April 2007

Targeting the Gatekeeper MET146 of C-Jun N-Terminal Kinase 3 Induces a Bivalent Halogen/Chalcogen Bond

scientific article

Targeting the Hinge Glycine Flip and the Activation Loop: Novel Approach to Potent p38α Inhibitors

scientific article published on August 29, 2012

Targeting the Protein Kinases Cysteinome.

scientific article published on 10 October 2017

Tetra-substituted pyridinylimidazoles as dual inhibitors of p38α mitogen-activated protein kinase and c-Jun N-terminal kinase 3 for potential treatment of neurodegenerative diseases

scientific article

Tetrasubstituted imidazole inhibitors of cytokine release: probing substituents in the N-1 position.

scientific article published in December 2004

The European Federation for Medicinal Chemistry (EFMC) Best Practice Initiative: Validating Chemical Probes

scientific article published on 03 September 2020

The Pyrazolobenzothiazine Core as a New Chemotype of p38 Alpha Mitogen-Activated Protein Kinase Inhibitors.

scientific article published on 14 January 2015

The decrease of cell membrane fluidity by the non-steroidal anti-inflammatory drug Licofelone inhibits epidermal growth factor receptor signalling and triggers apoptosis in HCA-7 colon cancer cells

scientific article

The dual inhibitor of lipoxygenase and cyclooxygenase ML3000 decreases the expression of CXCR3 ligands

scientific article published on 31 July 2007

The effect of single-dose naproxen on eicosanoid formation in human gastroduodenal mucosa

scientific article (publication date: 2006)

The effects of ML 3000 on antigen-induced responses in sheep

scientific article published on 01 June 1997

The gastrointestinal tolerability of the LOX/COX inhibitor, licofelone, is similar to placebo and superior to naproxen therapy in healthy volunteers: results from a randomized, controlled trial.

scientific article published in April 2004

The mechanism of action of the new antiinflammatory compound ML3000: inhibition of 5-LOX and COX-1/2.

scientific article

Three-component combinatorial synthesis of novel dihydropyrano[2,3-c]pyrazoles

scientific article published on 12 April 2008

Tofacitinib and analogs as inhibitors of the histone kinase PRK1 (PKN1).

scientific article

Treatment with licofelone prevents abnormal subchondral bone cell metabolism in experimental dog osteoarthritis

scientific article published on January 2004

Tri- and Tetrasubstituted Pyridinylimidazoles as Covalent Inhibitors of c-Jun N-Terminal Kinase 3.

scientific article published on 15 December 2016

Tri- and tetrasubstituted imidazoles as p38α mitogen-activated protein kinase inhibitors

scientific article published on September 9, 2010

Triggering of Suicidal Erythrocyte Death Following Boswellic Acid Exposure.

scientific article published on 17 August 2015

Triggering of Suicidal Erythrocyte Death by Ruxolitinib.

scientific article

Trisubstituted Imidazoles with a Rigidized Hinge Binding Motif Act As Single Digit nM Inhibitors of Clinically Relevant EGFR L858R/T790M and L858R/T790M/C797S Mutants: An Example of Target Hopping

scientific article published on 8 May 2017

Trisubstituted Pyridinylimidazoles as Potent Inhibitors of the Clinically Resistant L858R/T790M/C797S EGFR Mutant: Targeting of Both Hydrophobic Regions and the Phosphate Binding Site.

scientific article

Unexpected reaction of 2-alkylsulfanylimidazoles to imidazol-2-ones: pyridinylimidazol-2-ones as novel potent p38alpha mitogen-activated protein kinase inhibitors.

scientific article published in June 2010

Why Antidiabetic Vanadium Complexes are Not in the Pipeline of "Big Pharma" Drug Research? A Critical Review

scientific article

c-Jun N-terminal kinase inhibitors: a patent review (2010 - 2014).

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