77 articles for Z Yu
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Article Title
Organization
Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
Novartis Institutes For Biomedical Research
Discovery of high affinity inhibitors of Leishmania donovani N-myristoyltransferase.
Imperial College
Discovery of pyridyl-based inhibitors of Plasmodium falciparum N-myristoyltransferase.
Imperial College
Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers.
Leiden University
Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: success and challenges.
Zhengzhou University
When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists.
Leiden University
Discovery of 1-arylpyrrolidone derivatives as potent p53-MDM2 inhibitors based on molecule fusing strategy.
Second Military Medical University
Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists.
Leiden University
Strategies to reduce HERG K+ channel blockade. Exploring heteroaromaticity and rigidity in novel pyridine analogues of dofetilide.
Leiden University
Discovery of novel and ligand-efficient inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferase.
Imperial College
Design and synthesis of inhibitors of Plasmodium falciparum N-myristoyltransferase, a promising target for antimalarial drug discovery.
Imperial College
Novel enoyl-ACP reductase (FabI) potential inhibitors of Escherichia coli from Chinese medicine monomers.
Huazhong Agricultural University
Morin (3,5,7,2',4'-pentahydroxyflavone) exhibits potent inhibitory actions on urate transport by the human urate anion transporter (hURAT1) expressed in human embryonic kidney cells.
The Chinese University of Hong Kong
Salicylic acid based small molecule inhibitor for the oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2).
Indiana University School of Medicine
A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).
Icahn School of Medicine at Mount Sinai
Discovery of novel dihydropyrrolidone-thiadiazole compound crosstalk between the YycG/F two-component regulatory pathway and cell membrane homeostasis to combat methicillin-resistant Staphylococcus aureus.
Nanjing Tech University
Design, synthesis and biological evaluation of biaryl amide derivatives against SARS-CoV-2 with dual-target mechanism.
Chinese Academy of Medical Sciences and Peking Union Medical College
Design, Synthesis, and Biological Evaluation for First GPX4 and CDK Dual Inhibitors.
China Pharmaceutical University
Design, Synthesis and Antitumor Activity of a Novel Class of SHP2 Allosteric Inhibitors with a Furanyl Amide-Based Scaffold.
Shandong University
Small Molecule Targeting PPM1A Activates Autophagy for Mycobacterium tuberculosis Host-Directed Therapy.
Nanjing University of Chinese Medicine
Cyclic Peptide Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Design, Synthesis, and In Vivo Treatment of Acute Lung Injury.
Fujian University of Traditional Chinese Medicine
Design, synthesis and evaluation of C-5 substituted pyrrolopyridine derivatives as potent Janus Kinase 1 inhibitors with excellent selectivity.
University of South China
Chemical Catalysis Guides Structural Identification for the Major
Baylor College of Medicine
Recent progress toward developing axial chirality bioactive compounds.
Shandong University
Nitrile-containing pharmaceuticals: target, mechanism of action, and their SAR studies.
Tianjin University
Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.
Novartis Institutes For Biomedical Research
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities.
University of Arizona
Discovery of BP3 as an efficacious proteolysis targeting chimera (PROTAC) degrader of HSP90 for treating breast cancer.
Fujian Medical University (Fmu)
Novel Hybrids of 3-Substituted Coumarin and Phenylsulfonylfuroxan as Potent Antitumor Agents with Collateral Sensitivity against MCF-7/ADR.
Fudan University
Discovery of 2-(furan-2-ylmethylene)hydrazine-1-carbothioamide derivatives as novel inhibitors of SARS-CoV-2 main protease.
Peking University
Discovery of 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and selective CDK9 inhibitors that enable transient target engagement for the treatment of hematologic malignancies.
China Pharmaceutical University
Synthesis and biological evaluation of 4-(pyridine-4-oxy)-3-(tetrahydro-2H-pyran-4-yl)-pyrazole derivatives as novel, potent of ALK5 receptor inhibitors.
China Pharmaceutical University
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.
Activx Biosciences
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors.
Activx Biosciences
Discovery of Novel Histone Deacetylase 6 (HDAC6) Inhibitors with Enhanced Antitumor Immunity of Anti-PD-L1 Immunotherapy in Melanoma.
Southern Medical University
Synthesis and biological evaluation of 4-(pyridin-4-oxy)-3-(3,3-difluorocyclobutyl)-pyrazole derivatives as novel potent transforming growth factor-β type 1 receptor inhibitors.
China Pharmaceutical University
A potent photoreactive general anesthetic with novel binding site selectivity for GABA
University of Illinois At Chicago
Bifunctional and Unusual Amino Acid β- or γ-Ester Prodrugs of Nucleoside Analogues for Improved Affinity to ATB
Jiangxi University of Traditional Chinese Medicine
Synthesis of novel dual target inhibitors of PARP and HSP90 and their antitumor activities.
Fujian Medical University (Fmu)
Farnesyl Pyrophosphate Synthase as a Target for Drug Development: Discovery of Natural-Product-Derived Inhibitors and Their Activity in Pancreatic Cancer Cells.
Tsinghua University
Binding pocket-based design, synthesis and biological evaluation of novel selective BRD4-BD1 inhibitors.
Central South University
Structure-activity relationship studies on Bax activator SMBA1 for the treatment of ER-positive and triple-negative breast cancer.
University of Texas Medical Branch
Design, synthesis and biological evaluation of novel acetamide-substituted doravirine and its prodrugs as potent HIV-1 NNRTIs.
Shandong University
Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel.
Leiden University
Removal of human ether-à-go-go related gene (hERG) K+ channel affinity through rigidity: a case of clofilium analogues.
Leiden University
Difuran-substituted quinoxalines as a novel class of PI3Kα H1047R mutant inhibitors: Synthesis, biological evaluation and structure-activity relationship.
Chongqing University
Rational design of mitochondria-targeted pyruvate dehydrogenase kinase 1 inhibitors with improved selectivity and antiproliferative activity.
Chongqing University
Synthesis, biological evaluation and structure-activity relationship of a novel class of PI3Kα H1047R mutant inhibitors.
Chongqing University
Antiproliferative and apoptotic activities of sequence-specific histone acetyltransferase inhibitors.
Kyoto University
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
Discovery of Potent Small-Molecule Inhibitors of Ubiquitin-Conjugating Enzyme UbcH5c fromα-Santonin Derivatives.
Second Military Medical University
Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).
Icahn School of Medicine At Mount Sinai
Heteroaromatic amide derivative and medicament containing the same
Kaken Pharmaceutical Co.
S-CONFIGURATION-CONTAINING AMINO BENZAMIDE PYRIDAZINONE COMPOUND, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
Shanghai Institute of Materia Medica
4-ALKOXYPYRROLO[2,1-F][1,2,4]TRIAZINES AND PREPARATION AND USES THEREOF
Biosplice Therapeutics
5-substituted difluoropiperidine compounds with blood-brain barrier penetrable capability
Wayshine Biopharm Holding
Compositions and methods for the prevention and/or treatment of mitochondrial disease, including Friedreich's ataxia
Stealth Biotherapeutics
Combination of pure 5-HT6 receptor antagonists with acetylcholinesterase inhibitors
Suven Life Sciences
Substituted imidazoles as apoptosis signal regulating kinase 1 inhibitors
Jiangsu Hansoh Pharmaceutical Group
Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
Merck Sharpe & Dohme