152 articles for X Lu
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A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFR
Guangzhou Institutes of Biomedicine and Health
2-Aminopyrimidine Derivatives as New Selective Fibroblast Growth Factor Receptor 4 (FGFR4) Inhibitors.
Chinese Academy of Sciences
Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Ariad Pharmaceuticals
Design and synthesis of N-(4-aminopyridin-2-yl)amides as B-Raf(V600E) inhibitors.
Jilin University
Design, synthesis and anti-HIV evaluation of novel diarylpyridine derivatives targeting the entrance channel of NNRTI binding pocket.
Shandong University
Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant.
Guangzhou Institutes of Biomedicine and Health
Small molecule discoidin domain receptor kinase inhibitors and potential medical applications.
Chinese Academy of Sciences
Design, synthesis and evaluation of novel 2-(1H-imidazol-2-yl) pyridine Sorafenib derivatives as potential BRAF inhibitors and anti-tumor agents.
China Pharmaceutical University
Novel pyrazoline derivatives as bi-inhibitor of COX-2 and B-Raf in treating cervical carcinoma.
Second Affiliated Hospital of Southeast University
(±)-Torreyunlignans A-D, rare 8-9' linked neolignan enantiomers as phosphodiesterase-9A inhibitors from Torreya yunnanensis.
Sun Yat-Sen University
Synthesis of Deuterated Benzopyran Derivatives as Selective COX-2 Inhibitors with Improved Pharmacokinetic Properties.
Institutes of Biomedicine and Health
Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.
Shandong University
Identification and optimization of new dual inhibitors of B-Raf and epidermal growth factor receptor kinases for overcoming resistance against vemurafenib.
Chinese Academy of Sciences
Evaluation of aminohydantoins as a novel class of antimalarial agents.
Saint Louis University
Highly potent dipeptidyl peptidase IV inhibitors derived from Alogliptin through pharmacophore hybridization and lead optimization.
First Affiliated Hospital of Guangzhou Medical University
Discovery of potent dipeptidyl peptidase IV inhibitors through pharmacophore hybridization and hit-to-lead optimization.
Chinese Academy of Science
Discovery and optimization of 3-(2-(Pyrazolo[1,5-a]pyrimidin-6-yl)ethynyl)benzamides as novel selective and orally bioavailable discoidin domain receptor 1 (DDR1) inhibitors.
Chinese Academy of Sciences
Synthesis and biological evaluation of some novel resveratrol amide derivatives as potential anti-tumor agents.
Hefei University of Technology
Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors.
Ariad Pharmaceuticals
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.
Chinese Academy of Sciences
Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)¿isoleucine(315) mutant.
Chinese Academy of Sciences
Pharmacokinetic optimization of class-selective histone deacetylase inhibitors and identification of associated candidate predictive biomarkers of hepatocellular carcinoma tumor response.
Roche R & D Center China
Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups.
Washington University
Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity.
Nanjing University
Synthesis, biological evaluation, and molecular docking studies of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives as anticancer agents.
Nanjing University
Design, synthesis, and biological evaluation of novel conformationally constrained inhibitors targeting epidermal growth factor receptor threonine7¿°¿ methionine7¿° mutant.
Chinese Academy of Sciences
Novel pyrrolopyrimidine analogues as potent dipeptidyl peptidase IV inhibitors based on pharmacokinetic property-driven optimization.
Chinese Academy of Sciences
Structure-based design and synthesis of a novel class of Src SH2 inhibitors.
Ariad Pharmaceuticals
Design, synthesis and biological evaluation of N-phenylsulfonylnicotinamide derivatives as novel antitumor inhibitors.
Nanjing University
Synthesis, molecular modeling and biological evaluation of 2-(benzylthio)-5-aryloxadiazole derivatives as anti-tumor agents.
Nanjing University
Design and synthesis of 4,6-substituted-(diaphenylamino)quinazolines as potent EGFR inhibitors with antitumor activity.
Soochow University
Synthesis and biological evaluation of novel pyrimidine derivatives as sub-micromolar affinity ligands of GalR2.
The Scripps Research Institute
Design, synthesis and biological evaluation of pyridine acyl sulfonamide derivatives as novel COX-2 inhibitors.
Nanjing University
Metronidazole acid acyl sulfonamide: a novel class of anticancer agents and potential EGFR tyrosine kinase inhibitors.
Nanjing University
Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives as EGFR TK inhibitors and potential anticancer agents.
Nanjing University
Synthesis and in vitro biological evaluation of carbonyl group-containing analogues fors1 receptors.
Washington University
Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.
Washington University
Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.
Newcastle University
Application of p21 and klf2 reporter gene assays to identify selective histone deacetylase inhibitors for cancer therapy.
Roche R & D Center China
Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
Shanghai Hengrui Pharmaceuticals
Cell-active, irreversible covalent inhibitors that selectively target the catalytic lysine of EGFR by using fluorosulfate-based SuFEx chemistry.
National University of Singapore
Structure-Based Drug Design of 2-Amino-[1,1'-biphenyl]-3-carboxamide Derivatives as Selective PKMYT1 Inhibitors for the Treatment of CCNE1-Amplified Breast Cancer.
Jinan University
Targeting Solvent-Front Mutations for Kinase Drug Discovery: From Structural Basis to Design Strategies.
Jinan University
A Mitochondria-Targeting SIRT3 Inhibitor with Activity against Diffuse Large B Cell Lymphoma.
Cornell University
Drug Repurposing of ACT001 to Discover Novel Promising Sulfide Prodrugs with Improved Safety and Potent Activity for Neutrophil-Mediated Antifungal Immunotherapy.
Tongji University
Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach.
Nanjing University of Chinese Medicine
Discovery of Novel N-(Anthracen-9-ylmethyl) Benzamide Derivatives as ZNF207 Inhibitors Promising in Treating Glioma.
China Pharmaceutical University
Discovery of 6-Formylpyridyl Urea Derivatives as Potent Reversible-Covalent Fibroblast Growth Factor Receptor 4 Inhibitors with Improved Anti-Hepatocellular Carcinoma Activity.
Jinan University
Discovery of 4-benzylpiperazinequinoline BChE inhibitor that suppresses neuroinflammation for the treatment of Alzheimer's disease.
China Pharmaceutical University
Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy.
Jinan University
Development and Pharmacochemical Characterization Discover a Novel Brain-Permeable HDAC11-Selective Inhibitor with Therapeutic Potential by Regulating Neuroinflammation in Mice.
Sichuan University
Structure-Based Optimization of the Third Generation Type II Macrocycle TRK Inhibitors with Improved Activity against Solvent-Front, xDFG, and Gatekeeper Mutations.
Jinan University
Structural Mechanism and Inhibitors Targeting EGFR Exon 20 Insertion (Ex20ins) Mutations.
Jinan University
Design, Construction, and Screening of Diversified Pyrimidine-Focused DNA-Encoded Libraries.
Nanjing University of Chinese Medicine
Targeting MET: Discovery of Small Molecule Inhibitors as Non-Small Cell Lung Cancer Therapy.
Jinan University
Application of deep generative model for design of Pyrrolo[2,3-d] pyrimidine derivatives as new selective TANK binding kinase 1 (TBK1) inhibitors.
Jinan University
Discovery of orally active 1,4,5,6,8-pentaazaacenaphthylens as novel, selective, and potent covalent BTK inhibitors for the treatment of rheumatoid arthritis.
China Pharmaceutical University
Design, synthesis, and biological evaluation of aromatic tertiary amine derivatives as selective butyrylcholinesterase inhibitors for the treatment of Alzheimer's disease.
China Pharmaceutical University
Rational Design of Covalent Kinase Inhibitors by an Integrated Computational Workflow (Kin-Cov).
Jinan University
Discovery, SAR Study of GST Inhibitors from a Novel Quinazolin-4(1
Chinese Academy of Sciences
Biological Function of Pin1 in Vivo and Its Inhibitors for Preclinical Study: Early Development, Current Strategies, and Future Directions.
Shanghai University
Design, synthesis, and anti-inflammatory activity characterization of novel brain-permeable HDAC6 inhibitors.
Chinese Academy of Sciences
Privileged heterocycles for DNA-encoded library design and hit-to-lead optimization.
Chinese Academy of Sciences
Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1.
National Institute of Pharmaceutical Education and Research
Progress in PD-1/PD-L1 pathway inhibitors: From biomacromolecules to small molecules.
China Pharmaceutical University
Recent research progress of Uncaria spp. based on alkaloids: phytochemistry, pharmacology and structural chemistry.
China Pharmaceutical University
Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations.
Jinan University
Discovery of the First Highly Selective and Broadly Effective Macrocycle-Based Type II TRK Inhibitors that Overcome Clinically Acquired Resistance.
Jinan University
Design, Synthesis, and Biological Evaluation of Aminoindazole Derivatives as Highly Selective Covalent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR4.
Jinan University
The discovery of 1, 3-diamino-7H-pyrrol[3, 2-f]quinazoline compounds as potent antimicrobial antifolates.
Peking Union Medical College
-Benzyl Benzamide Derivatives as Selective Sub-Nanomolar Butyrylcholinesterase Inhibitors for Possible Treatment in Advanced Alzheimer's Disease.
China Pharmaceutical University
Discovery of a Novel Small-Molecule Inhibitor Disrupting TRBP-Dicer Interaction against Hepatocellular Carcinoma via the Modulation of microRNA Biogenesis.
Chinese Academy of Sciences
Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.
National Institute of Pharmaceutical Education and Research
Triazine-Based Covalent DNA-Encoded Libraries for Discovery of Covalent Inhibitors of Target Proteins.
Chinese Academy of Sciences
Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring
Jinan University
STING, a promising target for small molecular immune modulator: A review.
China Pharmaceutical University
Discovery of novel TrkA allosteric inhibitors: Structure-based virtual screening, biological evaluation and preliminary SAR studies.
Jinan University
Discovery of the First Examples of Threonine Tyrosine Kinase PROTAC Degraders.
Chinese Academy of Sciences
DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry.
Glaxosmithkline
Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors.
Guangzhou Institutes of Biomedicine and Health
Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold.
China Pharmaceutical University
Discovery of a Copper-Based Mcl-1 Inhibitor as an Effective Antitumor Agent.
Guangxi Normal University
Novel BuChE-IDO1 inhibitors from sertaconazole: Virtual screening, chemical optimization and molecular modeling studies.
Southwest University
Investigation of Covalent Warheads in the Design of 2-Aminopyrimidine-based FGFR4 Inhibitors.
Jinan University
Discovery of pyridine tetrahydroisoquinoline thiohydantoin derivatives with low blood-brain barrier penetration as the androgen receptor antagonists.
China Pharmaceutical University
Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics.
Jinan University
Medicinal Chemistry Strategies for the Development of Kinase Inhibitors Targeting Point Mutations.
Jinan University
A novel phosphotyrosine mimetic 4'-carboxymethyloxy-3'-phosphonophenylalanine (Cpp): exploitation in the design of nonpeptide inhibitors of pp60(Src) SH2 domain.
Ariad Pharmaceuticals
Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach.
Shandong University
Novel Lysine-Based Thioureas as Mechanism-Based Inhibitors of Sirtuin 2 (SIRT2) with Anticancer Activity in a Colorectal Cancer Murine Model.
TBA
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
Emory University
Structure-Based Design of Tetrahydroisoquinoline-7-carboxamides as Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.
Chinese Academy of Sciences
Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects.
Jinan University
Diketopiperazine-Type Alkaloids from a Deep-Sea-Derived Aspergillus puniceus Fungus and Their Effects on Liver X Receptor α.
Chinese Academy of Sciences
Discovery of naphthacemycins as a novel class of PARP1 inhibitors.
North China Pharmaceutical Group
Structure-Based Design of 5-Methylpyrimidopyridone Derivatives as New Wild-Type Sparing Inhibitors of the Epidermal Growth Factor Receptor Triple Mutant (EGFR
Jinan University
BH3 mimetics derived from Bim-BH3 domain core region show PTP1B inhibitory activity.
Ocean University of China
A-C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions.
Concordia University Wisconsin
Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.
Jinan University
Design, synthesis and biological evaluation of 3-(imidazo[1,2-a]pyrazin-3-ylethynyl)-2-methylbenzamides as potent and selective pan-tropomyosin receptor kinase (TRK) inhibitors.
Chinese Academy of Sciences
Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease.
Chinese Academy of Sciences
Design of Small Molecule Autophagy Modulators: A Promising Druggable Strategy.
China Pharmaceutical University
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
Shandong University
Transformation of monoamine oxidase-B primary amine substrates into time-dependent inhibitors. Tertiary amine homologues of primary amine substrates.
Northwestern University
Inactivation of monoamine oxidase B by analogues of the anticonvulsant agent milacemide (2-(n-pentylamino)acetamide).
Northwestern University
Design, synthesis, and biological evaluation of 2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl derivatives as new irreversible epidermal growth factor receptor inhibitors with improved pharmacokinetic properties.
Chinese Academy of Sciences
Synthesis, biological evaluation, and molecular docking studies of N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)aniline derivatives as novel anticancer agents.
Changzhou University
Design, synthesis and biological evaluation of novel (E)-α-benzylsulfonyl chalcone derivatives as potential BRAF inhibitors.
Nanjing University
The design and synthesis of N-1-alkylated-5-aminoarylalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors.
Peking University
Structure-based design of novel bicyclic nonpeptide inhibitors for the src SH2 domain.
Ariad Pharmaceuticals
Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-β agonists (SERBAs).
Marquette University
Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR.
Wuxi Apptec (Shanghai) Co.
Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ.
China Pharmaceutical University
The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2.
Shandong University
Investigation of multi-target-directed ligands (MTDLs) with butyrylcholinesterase (BuChE) and indoleamine 2,3-dioxygenase 1 (IDO1) inhibition: The design, synthesis of miconazole analogues targeting Alzheimer's disease.
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2.
Jinan University
Optimization of N-Substituted Oseltamivir Derivatives as Potent Inhibitors of Group-1 and -2 Influenza A Neuraminidases, Including a Drug-Resistant Variant.
Shandong University
Exploring the tetrahydroisoquinoline thiohydantoin scaffold blockade the androgen receptor as potent anti-prostate cancer agents.
China Pharmaceutical University
Isosteroidal alkaloids as potent dual-binding site inhibitors of both acetylcholinesterase and butyrylcholinesterase from the bulbs of Fritillaria walujewii.
Tianjin University of Technology
Varic acid analogues from fungus as PTP1B inhibitors: Biological evaluation and structure-activity relationships.
Dalian University of Technology
Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.
University of Macau
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
Shandong University
2-Oxo-3, 4-dihydropyrimido[4, 5-d]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors.
Guangzhou Institutes of Biomedicine and Health
Tetrahydroisoquinoline-7-carboxamide Derivatives as New Selective Discoidin Domain Receptor 1 (DDR1) Inhibitors.
Jinan University
Design, Synthesis, and Structure-Activity Relationship Study of 2-Oxo-3,4-dihydropyrimido[4,5- d]pyrimidines as New Colony Stimulating Factor 1 Receptor (CSF1R) Kinase Inhibitors.
Chinese Academy of Sciences
Discovery of Potent Small-Molecule Inhibitors of Ubiquitin-Conjugating Enzyme UbcH5c fromα-Santonin Derivatives.
Second Military Medical University
Inhibitors of RSV replication and applications thereof
Georgia State University Research Foundation
USE OF 5-[[4-[2-[5-ACETYLPYRIDIN-2-YL]ETHOXY]BENZYL]-1,3-THIAZOLIDINE-2,4-DIONE AND ITS SALTS
Minoryx Therapeutics
1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane X receptor
St. Jude Children''S Research Hospital
Matrix metalloproteinase inhibitors and methods for the treatment of pain and other diseases
TBA
Biological and structural evaluation of 10R- and 10S-methylthio-DDACTHF reveals a new role for sulfur in inhibition of glycinamide ribonucleotide transformylase.
The Scripps Research Institute
Characterization of a novel class of polyphenolic inhibitors of plasminogen activator inhibitor-1.
University of Michigan