Suchergebnisse - "Protein Kinase Inhibitors"

Protein Kinase Inhibitors: Synthesis and Molecular Repurposing in Three-Dimensional Cancer Models PKI.

Autoren: Lobanov V Rossomakhina N Kazakova E et al.

Quelle: Chemical biology & drug design [Chem Biol Drug Des] 2025 Nov; Vol. 106 (5), pp. e70195.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Wiley-Blackwell Country of Publication: England NLM ID: 101262549 Publication Model: Print Cited Medium: Internet ISSN: 1747-0285 (Electronic) Linking ISSN: 17470277 NLM ISO Abbreviation: Chem Biol Drug Des Subsets: MEDLINE

MeSH-Schlagworte: Protein Kinase Inhibitors*/chemical synthesis , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/therapeutic use , Drug Repositioning* , Neoplasms*/drug therapy , Neoplasms*/pathology , Neoplasms*/metabolism , Antineoplastic Agents*/chemical synthesis , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/therapeutic use, Humans ; Protein Kinases/metabolism ; Protein Kinases/chemistry

Dual ROCK1/2-MYLK4 Kinase Inhibition Preserves Visual Function in a Rat Model of Neuromyelitis Optica Spectrum Disorder Optic Neuritis.

Autoren: Huang CT Hossen M Chen TW et al.

Quelle: Cells [Cells] 2025 Oct 31; Vol. 14 (21). Date of Electronic Publication: 2025 Oct 31.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: MDPI Country of Publication: Switzerland NLM ID: 101600052 Publication Model: Electronic Cited Medium: Internet ISSN: 2073-4409 (Electronic) Linking ISSN: 20734409 NLM ISO Abbreviation: Cells Subsets: MEDLINE

MeSH-Schlagworte: rho-Associated Kinases*/antagonists & inhibitors , rho-Associated Kinases*/metabolism , Neuromyelitis Optica*/drug therapy , Neuromyelitis Optica*/physiopathology , Optic Neuritis*/drug therapy , Optic Neuritis*/physiopathology , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/therapeutic use , Vision, Ocular*/drug effects, Animals ; Rats ; Disease Models, Animal ; Rats, Sprague-Dawley ; Retinal Ganglion Cells/drug effects ; Retinal Ganglion Cells/pathology ; Retinal Ganglion Cells/metabolism ; Apoptosis/drug effects ; Aquaporin 4/metabolism ; Evoked Potentials, Visual/drug effects ; Optic Nerve/pathology ; Optic Nerve/drug effects ; Female ; Male

Successful use of enteric alectinib in a critically ill patient with metastatic ALK-adenocarcinoma: A case report.

Autoren: Braganca M Fernandes Pedro I Santos Nunes A et al.

Quelle: Pulmonology [Pulmonology] 2025 Dec 31; Vol. 31 (1), pp. 2523218. Date of Electronic Publication: 2025 Jul 02.

Publikationsart: Case Reports; Journal Article

Info zur Zeitschrift: Publisher: Taylor & Francis Country of Publication: United States NLM ID: 101723786 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 2531-0437 (Electronic) Linking ISSN: 25310429 NLM ISO Abbreviation: Pulmonology Subsets: MEDLINE

MeSH-Schlagworte: Piperidines*/administration & dosage , Piperidines*/therapeutic use , Carbazoles*/administration & dosage , Carbazoles*/therapeutic use , Lung Neoplasms*/drug therapy , Lung Neoplasms*/pathology , Lung Neoplasms*/genetics , Protein Kinase Inhibitors*/administration & dosage , Protein Kinase Inhibitors*/therapeutic use , Adenocarcinoma of Lung*/drug therapy , Adenocarcinoma*/drug therapy, Humans ; Anaplastic Lymphoma Kinase/genetics ; Critical Illness/therapy ; Male ; Treatment Outcome ; Adult

Small-molecule FGFR-targeted medicinal chemistry: Advances since 2020 and future perspectives.

Autoren: Yue H Wang Y Zhang N et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2025 Dec 15; Vol. 300, pp. 118117. Date of Electronic Publication: 2025 Sep 08.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Receptors, Fibroblast Growth Factor*/antagonists & inhibitors , Receptors, Fibroblast Growth Factor*/metabolism , Small Molecule Libraries*/chemistry , Small Molecule Libraries*/pharmacology , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemistry , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Neoplasms*/drug therapy , Neoplasms*/metabolism, Humans ; Chemistry, Pharmaceutical ; Molecular Structure ; Animals

Generation of a potent & selective series of IRAK4 inhibitors based on a structure based, hybridization approach.

Autoren: Terstiege I Aagaard A Berggren K et al.

Quelle: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2025 Dec 15; Vol. 131, pp. 118333. Date of Electronic Publication: 2025 Jul 28.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Interleukin-1 Receptor-Associated Kinases*/antagonists & inhibitors , Interleukin-1 Receptor-Associated Kinases*/metabolism , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemical synthesis, Humans ; Structure-Activity Relationship ; Molecular Structure ; Pyrazoles/chemistry ; Pyrazoles/pharmacology ; Pyrazoles/chemical synthesis ; Dose-Response Relationship, Drug ; Molecular Docking Simulation ; Pyridines/chemistry ; Pyridines/pharmacology

Design, synthesis, biological activity and molecular docking studies of triazolopyridine derivatives as ASK1 inhibitors.

Autoren: Su S Peng M Han X et al.

Quelle: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2025 Dec 15; Vol. 131, pp. 118417. Date of Electronic Publication: 2025 Sep 23.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE

MeSH-Schlagworte: MAP Kinase Kinase Kinase 5*/antagonists & inhibitors , MAP Kinase Kinase Kinase 5*/metabolism , Drug Design* , Molecular Docking Simulation* , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemical synthesis , Protein Kinase Inhibitors*/chemistry , Pyridines*/chemistry , Pyridines*/pharmacology , Pyridines*/chemical synthesis , Triazoles*/chemistry , Triazoles*/pharmacology , Triazoles*/chemical synthesis, Humans ; Structure-Activity Relationship ; Molecular Structure ; Dose-Response Relationship, Drug ; Cell Line

Design and synthesis of 4-azaindoles derivatives: targeting the cardiac troponin I-interacting kinase (TNNI3K).

Autoren: Chen K Sun M Ma K et al.

Quelle: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2025 Dec 15; Vol. 131, pp. 118395. Date of Electronic Publication: 2025 Sep 17.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Aza Compounds*/chemistry , Aza Compounds*/pharmacology , Aza Compounds*/chemical synthesis , Drug Design* , Indoles*/chemistry , Indoles*/pharmacology , Indoles*/chemical synthesis , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemical synthesis , Protein Kinase Inhibitors*/chemistry, Humans ; Dose-Response Relationship, Drug ; Molecular Dynamics Simulation ; Molecular Structure ; Myocytes, Cardiac/drug effects ; Quantitative Structure-Activity Relationship ; Protein Serine-Threonine Kinases

Discovery of N-(4-(pyridin-4-yloxy)phenyl)-1,2-dihydropyridine-3-carboxamide derivatives as potential type II c-Met inhibitors.

Autoren: Xin Q Fang C Xing B et al.

Quelle: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2025 Dec 15; Vol. 131, pp. 118394. Date of Electronic Publication: 2025 Sep 17.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Proto-Oncogene Proteins c-met*/antagonists & inhibitors , Proto-Oncogene Proteins c-met*/metabolism , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/chemical synthesis , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/chemical synthesis , Drug Discovery* , Dihydropyridines*/chemistry , Dihydropyridines*/pharmacology , Dihydropyridines*/chemical synthesis, Humans ; Cell Proliferation/drug effects ; Structure-Activity Relationship ; Apoptosis/drug effects ; Cell Line, Tumor ; Molecular Structure ; Drug Screening Assays, Antitumor ; Molecular Docking Simulation ; Dose-Response Relationship, Drug ; Cell Movement/drug effects

ATM inhibitors in cancer radiotherapy: Mechanisms, clinical development, and future directions.

Autoren: Al-Zoubi RM Garada K Al Huneidi R et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2025 Dec 15; Vol. 300, pp. 118137. Date of Electronic Publication: 2025 Sep 04.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Ataxia Telangiectasia Mutated Proteins*/antagonists & inhibitors , Ataxia Telangiectasia Mutated Proteins*/metabolism , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemistry , Neoplasms*/radiotherapy , Neoplasms*/drug therapy , Neoplasms*/metabolism , Neoplasms*/pathology , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Drug Development*, Humans ; Animals ; Molecular Structure

Structure activity relationship exploration of imidazo[1,2-a]pyridine series to reverse isoform selectivity and identify potent SIK1 selective inhibitors.

Autoren: Peixoto C De Lemos E Cherel L et al.

Quelle: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2025 Dec 15; Vol. 129, pp. 130397. Date of Electronic Publication: 2025 Sep 08.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE

MeSH-Schlagworte: Protein Serine-Threonine Kinases*/antagonists & inhibitors , Protein Serine-Threonine Kinases*/metabolism , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemical synthesis , Pyridines*/chemistry , Pyridines*/pharmacology , Pyridines*/chemical synthesis , Imidazoles*/chemistry , Imidazoles*/pharmacology , Imidazoles*/chemical synthesis, Structure-Activity Relationship ; Humans ; Molecular Structure ; Protein Isoforms/antagonists & inhibitors ; Protein Isoforms/metabolism ; Dose-Response Relationship, Drug

Targeting melanoma resistance: Novel oxindole and non-oxindole-based benzimidazole derivatives as potent dual inhibitors of BRAF ^V600E and ABL2 kinases.

Autoren: Badawy MAS Abdel-Aziz M Abdel-Rahman HM et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2025 Dec 15; Vol. 300, pp. 118096. Date of Electronic Publication: 2025 Aug 26.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Melanoma*/drug therapy , Melanoma*/pathology , Melanoma*/metabolism , Benzimidazoles*/pharmacology , Benzimidazoles*/chemistry , Benzimidazoles*/chemical synthesis , Proto-Oncogene Proteins B-raf*/antagonists & inhibitors , Proto-Oncogene Proteins B-raf*/metabolism , Proto-Oncogene Proteins B-raf*/genetics , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/chemical synthesis , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/chemical synthesis , Oxindoles*/chemistry , Oxindoles*/pharmacology , Oxindoles*/chemical synthesis , Drug Resistance, Neoplasm*/drug effects , Protein-Tyrosine Kinases*/antagonists & inhibitors , Protein-Tyrosine Kinases*/metabolism, Humans ; Structure-Activity Relationship ; Drug Screening Assays, Antitumor ; Molecular Structure ; Cell Proliferation/drug effects ; Cell Line, Tumor ; Dose-Response Relationship, Drug ; Molecular Docking Simulation ; Indoles/chemistry ; Indoles/pharmacology ; Apoptosis/drug effects

Identification of a novel Aurora B inhibitor using the AI-driven drug screening and docking-based traditional screening.

Autoren: Ye J Chen N Zhu Y et al.

Quelle: Bioorganic & medicinal chemistry [Bioorg Med Chem] 2025 Dec 15; Vol. 131, pp. 118423. Date of Electronic Publication: 2025 Sep 27.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Aurora Kinase B*/antagonists & inhibitors , Aurora Kinase B*/metabolism , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/chemical synthesis , Molecular Docking Simulation* , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/chemical synthesis, Humans ; Structure-Activity Relationship ; Molecular Structure ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Drug Evaluation, Preclinical ; Cell Proliferation/drug effects ; Cell Line, Tumor ; Machine Learning

Overcoming EGFR mutation resistance: Dual inhibition strategies using TKIs in non-small cell lung cancer therapy.

Autoren: Sivam J Ariffin A Sinniah A et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2025 Dec 15; Vol. 300, pp. 118135. Date of Electronic Publication: 2025 Sep 12.

Publikationsart: Journal Article; Review

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Carcinoma, Non-Small-Cell Lung*/drug therapy , Carcinoma, Non-Small-Cell Lung*/metabolism , Carcinoma, Non-Small-Cell Lung*/pathology , Carcinoma, Non-Small-Cell Lung*/genetics , Lung Neoplasms*/drug therapy , Lung Neoplasms*/pathology , Lung Neoplasms*/metabolism , Lung Neoplasms*/genetics , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemistry , Drug Resistance, Neoplasm*/drug effects , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry, Humans ; ErbB Receptors/genetics ; ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/metabolism ; Mutation/drug effects ; Molecular Structure

Aurora A degradation by HSP90 interactome-mediating PROTACs in A549 and paclitaxel-resistant A549 cells.

Autoren: Deng XY Xu H Peng YX et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2025 Dec 15; Vol. 300, pp. 118141. Date of Electronic Publication: 2025 Sep 06.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: HSP90 Heat-Shock Proteins*/metabolism , HSP90 Heat-Shock Proteins*/antagonists & inhibitors , Aurora Kinase A*/metabolism , Aurora Kinase A*/antagonists & inhibitors , Paclitaxel*/pharmacology , Paclitaxel*/chemistry , Drug Resistance, Neoplasm*/drug effects , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/chemical synthesis , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/chemical synthesis, Humans ; Animals ; Cell Proliferation/drug effects ; Mice ; A549 Cells ; Lung Neoplasms/drug therapy ; Lung Neoplasms/pathology ; Lung Neoplasms/metabolism ; Proteolysis/drug effects ; Molecular Structure ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Structure-Activity Relationship ; Mice, Nude ; Proteolysis Targeting Chimera

Microwave-assisted one-pot green synthesis, ADMET profiling, DFT, and molecular docking of novel 3-cyano-2-pyridone derivatives as dual EGFR and cytokine (TNF-α, IL-6) inhibitors.

Autoren: Lotfy EM Bokhtia RM Abdel Fattah HA et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2025 Dec 15; Vol. 300, pp. 118165. Date of Electronic Publication: 2025 Sep 15.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Molecular Docking Simulation* , Interleukin-6*/antagonists & inhibitors , Interleukin-6*/metabolism , Tumor Necrosis Factor-alpha*/antagonists & inhibitors , Tumor Necrosis Factor-alpha*/metabolism , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemical synthesis , Antineoplastic Agents*/chemistry , Pyridones*/pharmacology , Pyridones*/chemistry , Pyridones*/chemical synthesis , Microwaves* , Density Functional Theory* , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemical synthesis , Protein Kinase Inhibitors*/chemistry, Humans ; ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/metabolism ; Molecular Structure ; Structure-Activity Relationship ; Drug Screening Assays, Antitumor ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Green Chemistry Technology ; Apoptosis/drug effects ; Cell Survival/drug effects

Discovery of a novel benzofuran-7-carboxamide-based PARP1/c-Met dual inhibitor for addressing c-Met amplification-mediated PARP1i acquired-resistance.

Autoren: Sun Z Hu M Xu J et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2025 Dec 15; Vol. 300, pp. 118164. Date of Electronic Publication: 2025 Sep 14.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Proto-Oncogene Proteins c-met*/antagonists & inhibitors , Proto-Oncogene Proteins c-met*/metabolism , Benzofurans*/chemistry , Benzofurans*/pharmacology , Benzofurans*/chemical synthesis , Poly (ADP-Ribose) Polymerase-1*/antagonists & inhibitors , Poly (ADP-Ribose) Polymerase-1*/metabolism , Poly(ADP-ribose) Polymerase Inhibitors*/pharmacology , Poly(ADP-ribose) Polymerase Inhibitors*/chemistry , Poly(ADP-ribose) Polymerase Inhibitors*/chemical synthesis , Drug Resistance, Neoplasm*/drug effects , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/chemical synthesis , Drug Discovery* , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/chemical synthesis, Humans ; Structure-Activity Relationship ; Animals ; Molecular Structure ; Mice ; Cell Proliferation/drug effects ; Drug Screening Assays, Antitumor ; Dose-Response Relationship, Drug

The synthesis and evaluation of new N-(pyrazin-2-yl)-4-aminopyrimidine derivatives targeted EGFR and JAK.

Autoren: Yao H Cao L Ma EE et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2025 Dec 15; Vol. 300, pp. 118120. Date of Electronic Publication: 2025 Sep 08.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemical synthesis , Antineoplastic Agents*/chemistry , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemical synthesis , Protein Kinase Inhibitors*/chemistry , Janus Kinase 2*/antagonists & inhibitors , Janus Kinase 2*/metabolism , Pyrimidines*/pharmacology , Pyrimidines*/chemistry , Pyrimidines*/chemical synthesis , Janus Kinase 3*/antagonists & inhibitors , Janus Kinase 3*/metabolism , Pyrazines*/pharmacology , Pyrazines*/chemistry , Pyrazines*/chemical synthesis, Humans ; ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/metabolism ; Animals ; Mice ; Structure-Activity Relationship ; Molecular Structure ; Drug Screening Assays, Antitumor ; Mice, Nude ; Cell Proliferation/drug effects ; Dose-Response Relationship, Drug ; Cell Line, Tumor ; Neoplasms, Experimental/drug therapy ; Neoplasms, Experimental/pathology ; Neoplasms, Experimental/metabolism

Discovery of novel 3-Benzyloxyaminopyridines as orally available and intracranially active selective ROS1 inhibitors for combating the resistant ROS1 ^G2032R mutation.

Autoren: Liu S Tian Y Huang Y et al.

Quelle: European journal of medicinal chemistry [Eur J Med Chem] 2025 Dec 15; Vol. 300, pp. 118089. Date of Electronic Publication: 2025 Aug 26.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Editions Scientifiques Elsevier Country of Publication: France NLM ID: 0420510 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1768-3254 (Electronic) Linking ISSN: 02235234 NLM ISO Abbreviation: Eur J Med Chem Subsets: MEDLINE

MeSH-Schlagworte: Proto-Oncogene Proteins*/antagonists & inhibitors , Proto-Oncogene Proteins*/genetics , Proto-Oncogene Proteins*/metabolism , Aminopyridines*/pharmacology , Aminopyridines*/chemistry , Aminopyridines*/administration & dosage , Aminopyridines*/chemical synthesis , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/administration & dosage , Protein Kinase Inhibitors*/chemical synthesis , Protein-Tyrosine Kinases*/antagonists & inhibitors , Protein-Tyrosine Kinases*/genetics , Protein-Tyrosine Kinases*/metabolism , Antineoplastic Agents*/pharmacology , Antineoplastic Agents*/chemistry , Antineoplastic Agents*/administration & dosage , Antineoplastic Agents*/chemical synthesis , Drug Discovery*, Humans ; Animals ; Mutation ; Administration, Oral ; Structure-Activity Relationship ; Molecular Structure ; Mice ; Dose-Response Relationship, Drug ; Cell Proliferation/drug effects ; Drug Screening Assays, Antitumor ; Cell Line, Tumor ; Drug Resistance, Neoplasm/drug effects

Discovery of GLPG4471, a potent and selective IRAK4 inhibitor for the treatment of inflammatory and autoimmune diseases.

Autoren: Mammoliti O Bonnaterre F Newsome G et al.

Quelle: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2025 Dec 15; Vol. 129, pp. 130386. Date of Electronic Publication: 2025 Aug 23.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE

MeSH-Schlagworte: Interleukin-1 Receptor-Associated Kinases*/antagonists & inhibitors , Interleukin-1 Receptor-Associated Kinases*/metabolism , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/therapeutic use , Protein Kinase Inhibitors*/chemical synthesis , Autoimmune Diseases*/drug therapy , Drug Discovery* , Arthritis, Experimental*/drug therapy , Inflammation*/drug therapy, Animals ; Humans ; Mice ; Structure-Activity Relationship ; Molecular Structure ; Dose-Response Relationship, Drug

Discovery of A20 with 4-(2-methoxyphenyl)-1H-pyrazole scaffold as a potent and selective ROCK2 inhibitor.

Autoren: Wang J Peng B Liang G et al.

Quelle: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2025 Dec 15; Vol. 129, pp. 130391. Date of Electronic Publication: 2025 Aug 29.

Publikationsart: Journal Article

Info zur Zeitschrift: Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE

MeSH-Schlagworte: rho-Associated Kinases*/antagonists & inhibitors , rho-Associated Kinases*/metabolism , Pyrazoles*/chemistry , Pyrazoles*/pharmacology , Pyrazoles*/chemical synthesis , Protein Kinase Inhibitors*/chemistry , Protein Kinase Inhibitors*/pharmacology , Protein Kinase Inhibitors*/chemical synthesis , Drug Discovery*, Structure-Activity Relationship ; Humans ; Molecular Docking Simulation ; Molecular Structure ; Dose-Response Relationship, Drug