Keywords: انتخابی کیناز; JAK2 inhibitor; 4-(2-Furanyl)pyrimidin-2-amine; 4,5,6,7-Tetrahydro-furo[3,2-c]pyridine; Kinase selectivity;
مقالات ISI انتخابی کیناز (ترجمه نشده)
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Keywords: انتخابی کیناز; TNNI3K; B-Raf; Quinazoline; Substituent effects; Kinase selectivity
Discovery of 4-ethoxy-7H-pyrrolo[2,3-d]pyrimidin-2-amines as potent, selective and orally bioavailable LRRK2 inhibitors
Keywords: انتخابی کیناز; Pyrrolo[2,3-d]pyrimidine; LRRK2; Parkinson's disease; Kinase selectivity; CNS penetration;
Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology
Keywords: انتخابی کیناز; ERK inhibitor; ATP competitive; MAP kinases; Kinase selectivity; Oncology;
Design and synthesis of novel pyrimidine analogs as highly selective, non-covalent BTK inhibitors
Keywords: انتخابی کیناز; Bruton's tyrosine kinase; Kinase inhibitor; Kinase selectivity; Pyrimidine; Passive cutaneous anaphylaxis;
Synthesis and SAR of 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivatives as potent and selective CDK4/6 inhibitors
Keywords: انتخابی کیناز; Cyclin dependent kinase; Anticancer; Cell cycle; Kinase selectivity;
Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis
Keywords: انتخابی کیناز; BTK inhibitor; ATP ribose pocket; Rheumatoid arthritis; Kinase selectivity; Immunology;
Discovery of a novel aminopyrazine series as selective PI3Kα inhibitors
Keywords: انتخابی کیناز; PI3Kα inhibitor; Rational design; Kinase selectivity;
Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors
Keywords: انتخابی کیناز; Parkinson's disease; LRRK2 inhibitor; Arylbenzamide; CNS penetration; Kinase selectivity;
Discovery and evaluation of 1H-pyrrolo[2,3-b]pyridine based selective and reversible small molecule BTK inhibitors for the treatment of rheumatoid arthritis
Keywords: انتخابی کیناز; BTK; Reversible; 1H-Pyrrolo[2,3-b]pyridine; Human whole blood; Kinase selectivity; Autoimmune diseases; Rheumatoid arthritis;
Multi-step virtual screening to develop selective DYRK1A inhibitors
Keywords: انتخابی کیناز; DYRK1A; Kinase selectivity; In silico screening; Free energy decomposition; Discriminant analysis;
Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK)
Keywords: انتخابی کیناز; SYK; Kinase inhibitor; Kinase selectivity; Structure-based drug discovery; Leukemia; Lymphoma;
Development of a potent and selective FLT3 kinase inhibitor by systematic expansion of a non-selective fragment-screening hit
Keywords: انتخابی کیناز; FLT3; Kinase inhibitor; Kinase selectivity; Fragment based drug discovery; Acute myeloid leukemia
Discovery of a potent and highly selective transforming growth factor β receptor-associated kinase 1 (TAK1) inhibitor by structure based drug design (SBDD)
Keywords: انتخابی کیناز; TAK1; SBDD; Inhibitor; Kinase selectivity
Discovery and antiplatelet activity of a selective PI3Kβ inhibitor (MIPS-9922)
Keywords: انتخابی کیناز; PI3 kinase; Kinase selectivity; Platelet aggregation inhibitors; ThrombosisACD, Acid citrate dextrose; PTEN, phosphatase and tensin homolog; ADME, absorption, distribution, metabolism, and excretion; TRAP, thrombin receptor activating peptide; PRP, platel
Synthesis and biological evaluation of N-cyclopropylbenzamide-benzophenone hybrids as novel and selective p38 mitogen activated protein kinase (MAPK) inhibitors
Keywords: انتخابی کیناز; N-Cyclopropylbenzamide; P38 mitogen activated protein kinase inhibitor; Benzophenone; Hybrid; Kinase selectivity
Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: Success and challenges
Keywords: انتخابی کیناز; Spirooxindoles; CFI-400945; Anticancer drug; Kinase selectivity;
Design of selective PI3Kα inhibitors starting from a promiscuous pan kinase scaffold
Keywords: انتخابی کیناز; PI3Kα inhibitor; Kinase selectivity;
Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton’s tyrosine kinase (BTK) inhibitors
Keywords: انتخابی کیناز; BTK inhibitors; Thieno[3,2-c]pyrid-4-amine; Inhibitory activity; Kinase selectivity
Discovery of 4-arylamido 3-methyl isoxazole derivatives as novel FMS kinase inhibitors
Keywords: انتخابی کیناز; 4-arylamido 3-methyl isoxazoles; Antiproliferative activity; Hematopoietic cell line; Kinase inhibitor; Kinase selectivity;
Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors
Keywords: انتخابی کیناز; BTK inhibitors; Thieno[3,2-c]pyridin-4-amine; Inhibitory activity; Kinase selectivity;
The discovery of reverse tricyclic pyridone JAK2 inhibitors. Part 2: Lead optimization
Keywords: انتخابی کیناز; JAK2; Kinases; Water interaction; Kinase selectivity; Ligand binding affinity; Kinase partition index; Molecular modeling;
Identification of protein binding partners of ALK-5 kinase inhibitors
Keywords: انتخابی کیناز; Transforming growth factor β-1; Activin-like kinase-5; Kinase inhibitor; Kinase selectivity; Affinity chromatography;
Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): Kinase profiling guided optimization of a 1,2,3-benzotriazole lead
Keywords: انتخابی کیناز; NXWXUDHOUKWAQU-MEMLXQNLSA-N; JSQNZBQJTQNCFK-JOCQHMNTSA-N; DPTBYUQHDCZBPL-HDJSIYSDSA-N; QTUUSRHXDAHSAU-WKILWMFISA-N; JNK; c-Jun N-terminal kinase; MAP; mitogen-activated protein; CDK-2; cyclin-dependent kinase-2; c-Jun N-terminal kinase (JNK); CDK; Kinase
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome
Keywords: انتخابی کیناز; Kinase inhibitors; Janus kinase; JAK; Structure based design; Kinase selectivity; Conformational bias;
Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones
Keywords: انتخابی کیناز; ERK5 inhibitor; Kinase selectivity; Benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-one; BMK1; big MAP kinase 1; DIEA; N,N-diisopropylethylamine; DCAMKL2; doublecortin and CaM kinase-like 2; DMA; N,N-dimethylacetamide; EGF; epidermal growth factor; ERK5; extrace
Discovery and optimization of pyrrolo[1,2-a]pyrazinones leads to novel and selective inhibitors of PIM kinases
Keywords: انتخابی کیناز; PIM kinases; Natural product scaffold; Pyrrolopyrazinone; Kinase selectivity; Anti-cancer agents;
Pyrazolopyridine inhibitors of B-RafV600E. Part 4: Rational design and kinase selectivity profile of cell potent type II inhibitors
Keywords: انتخابی کیناز; B-RafV600E; Inactive conformation; DFG-out; Structure-based design; Kinase selectivity;
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors
Keywords: انتخابی کیناز; Mps1 kinase; TTK kinase; Lead optimization; Cancer; Kinase selectivity;
Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases
Keywords: انتخابی کیناز; Pim-kinase inhibitors; Indole; Kinase selectivity; Oncology
Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors
Keywords: انتخابی کیناز; MPS1; TTK; Anticancer; Kinase selectivity; SAR
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells
Keywords: انتخابی کیناز; Dihydropyrazolodiazepinone; Antiproliferative activity; Cancer cell line; Kinase inhibitor; Kinase selectivity;
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells
Keywords: انتخابی کیناز; Aminopyrazole amide; Antiproliferative activity; Melanoma cell line; Kinase inhibitor; Kinase selectivity;
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors
Keywords: انتخابی کیناز; JNK; c-Jun N-terminal kinase; Diabetes, pyrimidine, pyrazole; Kinase selectivity
Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR
Keywords: انتخابی کیناز; p38 kinase; p38α; p38; CSBP; MAP kinase; Inhibitors; BPA, biphenyl amide; BPAs, biphenyl amides; Protein kinase X-ray structure; Binding mode; Structure-based drug design; Kinase selectivity
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity
Keywords: انتخابی کیناز; p38 Kinase; p38 Alpha; p38; CSBP; MAP kinase; Inhibitors; Biphenyl amide; BPA; Biphenyl amides; BPAs; Protein kinase X-ray structure; Binding mode; Structure-based drug design; Kinase selectivity; Structure–activity relationships; PG-PS model; CIA model
Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode
Keywords: انتخابی کیناز; p38 kinase; p38 alpha; p38; CSBP; MAP kinase; Inhibitors; Biphenyl amide; BPA; Biphenyl amides; BPAs; Protein kinase X-ray structure; Binding mode; Pharmacophore search; Focused screen; Virtual screening; Structure-based drug design; kinase selectivity
A practical synthesis of the major 3-hydroxy-2-pyrrolidinone metabolite of a potent CDK2/cyclin A inhibitor
Keywords: انتخابی کیناز; CDK2; Cyclins; Kinase selectivity; Tumour cell proliferation inhibition; Polymer-assisted solution-phase synthesis; Polymer-supported reagents;
Tricyclic azepine derivatives: Pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors
Keywords: انتخابی کیناز; Epidermal growth factor receptor; Kinase inhibitor; Benzoxazepine; Kinase selectivity
Benzodipyrazoles: a new class of potent CDK2 inhibitors
Keywords: انتخابی کیناز; CDK2; Cyclins; Kinase selectivity; Tumor cell proliferation inhibition;