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Article Title
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Design, synthesis and biological evaluation of quinazoline-phosphoramidate mustard conjugates as anticancer drugs.

Peking University
Comparison of the inhibition of Escherichia coli and Lactobacillus casei dihydrofolate reductase by 2,4-diamino-5-(substituted-benzyl)pyrimidines: quantitative structure-activity relationships, X-ray crystallography, and computer graphics in structure-activity analysis.

TBA
A comparison of the inhibitory action of 5-(substituted-benzyl)-2,4-diaminopyrimidines on dihydrofolate reductase from chicken liver with that from bovine liver.

TBA
Novel bicyclo[3.1.0]hexane analogs as antagonists of metabotropic glutamate 2/3 receptors for the treatment of depression.

Eli Lilly
Structure-Based Identification of Novel Ligands Targeting Multiple Sites within a Chemokine-G-Protein-Coupled-Receptor Interface.

University of South Florida
Design and optimization of novel 4-(2-fluorophenoxy)quinoline derivatives bearing a hydrazone moiety as c-Met kinase inhibitors.

Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors.

Peking University
Novel pyrazole-5-carboxamide and pyrazole-pyrimidine derivatives: synthesis and anticancer activity.

Anhui Medical University
Design, synthesis and evaluation of marinopyrrole derivatives as selective inhibitors of Mcl-1 binding to pro-apoptotic Bim and dual Mcl-1/Bcl-xL inhibitors.

University of Nebraska
Design, synthesis and biological evaluation of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 4-oxo-3,4-dihydrophthalazine-1-carboxamide moieties as c-Met kinase inhibitors.

Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives possessing diaryl semicarbazone scaffolds as potent antitumor agents.

Shenyang Pharmaceutical University
Discovery andw biological evaluation of novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety as c-Met kinase inhibitors.

Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University)
Fast identification of novel lymphoid tyrosine phosphatase inhibitors using target-ligand interaction-based virtual screening.

Shandong University
Discovery of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing 5-(aminomethylene)pyrimidine-2,4,6-trione moiety as c-Met kinase inhibitors.

Shenyang Pharmaceutical University
Self-organizing molecular field analysis on humanß-secretase nonpeptide inhibitors: 5, 5-disubstituted aminohydantoins.

Sichuan University
Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors.

H. Lee Moffitt Cancer Center and Research Institute
Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.

University of South Florida
4-aminopyrimidine-5-carbaldehyde oximes as potent VEGFR-2 inhibitors. Part II.

Johnson & Johnson Pharmaceutical Research & Development
Structure-activity relationships in toll-like receptor-2 agonistic diacylthioglycerol lipopeptides.

University of Kansas
Discovery of highly potent and selective VEGFR2 kinase inhibitors for the treatment of rheumatoid arthritis.

Anhui Medical University
Design, synthesis and biological evaluation of indazole derivatives as VEGFR-2 kinase inhibitors with anti-angiogenic properties.

Anhui Medical University
Recent advances in the exploration of oxazolidinone scaffolds from compound development to antibacterial agents and other bioactivities.

Zhengzhou University
Discovery of CBPD-268 as an Exceptionally Potent and Orally Efficacious CBP/p300 PROTAC Degrader Capable of Achieving Tumor Regression.

University of Michigan
Discovery of (R)-4-(8-methoxy-2-methyl-1-(1-phenylethy)-1H-imidazo[4,5-c]quinnolin-7-yl)-3,5-dimethylisoxazole as a potent and selective BET inhibitor for treatment of acute myeloid leukemia (AML) guided by FEP calculation.

Sichuan University
Design, Synthesis and Antitumor Activity of a Novel Class of SHP2 Allosteric Inhibitors with a Furanyl Amide-Based Scaffold.

Shandong University
Design, synthesis and antitumor activity of 4-arylamine substituted pyrimidine derivatives as noncovalent EGFR inhibitors overcoming C797S mutation.

Guizhou University
Targeted regulated cell death with small molecule compounds in colorectal cancer: Current perspectives of targeted therapy and molecular mechanisms.

Sichuan University
Discovery of Novel Proteolysis-Targeting Chimera Molecules as Degraders of Programmed Cell Death-Ligand 1 for Breast Cancer Therapy.

Sichuan University
Discovery of novel diaryl substituted isoquinolin-1(2H)-one derivatives as hypoxia-inducible factor-1 signaling inhibitors for the treatment of rheumatoid arthritis.

Anhui Medical University
Drug repurposing of propafenone to discover novel anti-tumor agents by impairing homologous recombination to delay DNA damage recovery of rare disease conjunctival melanoma.

East China University of Science and Technology
Design, synthesis and biological evaluation of 2,4,6- trisubstituted triazine derivatives as new nonpeptide small-molecule SIRT5 inhibitors.

Xihua University
Structure-Activity Relationship Study of 1

University of Chinese Academy of Sciences
Structure-Activity Relationship Studies of 2,4,5-Trisubstituted Pyrimidine Derivatives Leading to the Identification of a Novel and Potent Sirtuin 5 Inhibitor against Sepsis-Associated Acute Kidney Injury.

Xihua University
Design, Synthesis, and Biological Evaluation of New 1H-Imidazole-2-Carboxylic Acid Derivatives as Metallo-β-Lactamase Inhibitors.

Xihua University
Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).

Johnson & Johnson Pharmaceutical Research & Development
Recent advances in β-lactamase inhibitor chemotypes and inhibition modes.

Xihua University
Discovery of the GSH responsive "Y-PROTACs" targeting ALK and CDK4/6 as a potential treatment for cancer.

West China Hospital of Sichuan University
Design, Synthesis, and Biological Evaluation of Bipyridazine Derivatives as Stimulator of Interferon Genes (STING) Receptor Agonists.

Fudan University
Rho Kinase (ROCK) Inhibitors and Their Therapeutic Potential.

Amakem Therapeutics
Discovery of a Potent, Cooperative, and Selective SOS1 PROTAC ZZ151 with In Vivo Antitumor Efficacy in KRAS-Mutant Cancers.

Shanghai Institute of Materia Medica
Structure-activity relationships of Wee1 inhibitors: A review.

Sichuan University
Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors.

Johnson & Johnson Pharmaceutical Research & Development
Selective degradation of PARP2 by PROTACs via recruiting DCAF16 for triple-negative breast cancer.

West China Hospital of Sichuan University
Design and synthesis of 5-aryl-pyridone-carboxamides as inhibitors of anaplastic lymphoma kinase.

Chembridge Research Laboratories and Chembridge
Design, synthesis and structure-activity relationship studies of pyrido[2,3-d]pyrimidin-7-ones as potent Janus Kinase 3 (JAK3) covalent inhibitors.

Chinese Academy of Sciences
Design, synthesis, and biological evaluation of novel (4-(1,2,4-oxadiazol-5-yl)phenyl)-2-aminoacetamide derivatives as multifunctional agents for the treatment of Alzheimer's disease.

Anhui Medical University
Synthesis and biological evaluation of a tumor-selective degrader of PARP1.

West China Hospital of Sichuan University
Discovery of 2-Methyl-2-(4-(2-methyl-8-(1

West China Hospital of Sichuan University
Drug Repurposing of Quisinostat to Discover Novel

East China University of Science and Technology
Identification of a Novel TAR RNA-Binding Protein 2 Modulator with Potential Therapeutic Activity against Hepatocellular Carcinoma.

Chinese Academy of Sciences
N-(4-acetamidophenyl)-5-acetylfuran-2-carboxamide as a novel orally available diuretic that targets urea transporters with improved PD and PK properties.

Peking University
Elucidation of Distinct Modular Assemblies of Smoothened Receptor by Bitopic Ligand Measurement.

Shanghaitech University
Discovery of new human Sirtuin 5 inhibitors by mimicking glutaryl-lysine substrates.

Xihua University
Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression.

University of Tennessee Health Science Center
Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold.

Sichuan University
Discovery of new tranylcypromine derivatives as highly potent LSD1 inhibitors.

Zhengzhou University
Discovery of a PROTAC targeting ALK with in vivo activity.

West China Hospital of Sichuan University
Discovery of

Peking Union Medical College
Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.

Centro De Investigaci£N Lilly S.A. Avda. De La Industria
SD-91 as A Potent and Selective STAT3 Degrader Capable of Achieving Complete and Long-Lasting Tumor Regression.

University of Michigan
Discovery of Novel

East China University of Science and Technology
Targeting Cysteine Located Outside the Active Site: An Effective Strategy for Covalent ALKi Design.

West China Hospital of Sichuan University
A bicyclic pentapeptide-based highly potent and selective pan-SIRT1/2/3 inhibitor harboring N

Fudan University
EEDi-5285: An Exceptionally Potent, Efficacious, and Orally Active Small-Molecule Inhibitor of Embryonic Ectoderm Development.

University of Michigan
Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs).

School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.

Chengdu University
Discovery of 4-phenyl-2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as potent and orally active PI3K/mTOR dual inhibitors.

West China Hospital of Sichuan University
Identification of Ezetimibe and Pranlukast as Pharmacological Chaperones for the Treatment of the Rare Disease Mucopolysaccharidosis Type IVA.

Universidad Nacional De Colombia
Synthesis and anti-tumor efficacy of novel 2, 4-diarylaminopyrimidine derivatives bearing N-(3-pyridinylmethyl) urea moiety as anaplastic lymphoma kinase inhibitors.

Peking University Health Science Center
Discovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1α Signaling Inhibitors with Potent Activities of Anticancer Metastasis.

Anhui Medical University
Drugs for the Treatment of Zika Virus Infection.

University of North Carolina at Chapel Hill
Discovery of 2,4-diarylaminopyrimidine derivatives bearing dithiocarbamate moiety as novel FAK inhibitors with antitumor and anti-angiogenesis activities.

Peking University Health Science Center
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors.

Peking University Health Science Center
Discovery and optimization of thienopyridine derivatives as novel urea transporter inhibitors.

Peking University
Structure-based design and synthesis of lipophilic 2,4-diamino-6-substituted quinazolines and their evaluation as inhibitors of dihydrofolate reductases and potential antitumor agents.

Duquesne University
Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency.

Dupont Pharmaceuticals
Kinase and Histone Deacetylase Hybrid Inhibitors for Cancer Therapy.

Qingdao University
Identification of selective and reversible LSD1 inhibitors with anti-metastasis activity by high-throughput docking.

Taizhou People'S Hospital
Discovery of Irreversible Inhibitors Targeting Histone Methyltransferase, SMYD3.

Experimental Drug Development Centre
PB-10, a thiazolo[4,5-d] pyrimidine derivative, targets p21-activated kinase 4 in human colorectal cancer cells.

Inner Mongolia Medical University
Synthetic bicyclic iminosugar derivatives fused thiazolidin-4-one as new potential HIV-RT inhibitors.

Hebei University
Inhibition by 5-(substituted-benzyl)-2,4-diaminopyrimidines of murine tumor (L5178Y) cell cultures sensitive to and resistant to methotrexate. Further evidence for the sensitivity of resistant cells to hydrophobic drugs.

TBA
Synthesis and biological evaluation of curcumin derivatives modified with α-amino boronic acid as proteasome inhibitors.

Peking University
Bioactive Glycosides from the Twigs of Litsea cubeba.

Lanzhou University
The discovery and optimization of naphthalene-linked P2-P4 Macrocycles as inhibitors of HCV NS3 protease.

Bristol-Myers Squibb
Bysspectin A, an unusual octaketide dimer and the precursor derivatives from the endophytic fungus Byssochlamys spectabilis IMM0002 and their biological activities.

Peking Union Medical College
Discovery of Highly Potent Pinanamine-Based Inhibitors against Amantadine- and Oseltamivir-Resistant Influenza A Viruses.

School of Pharmaceutical Sciences & The Fifth Affiliated Hospital
Discovery of novel naphthoquinone derivatives as inhibitors of the tumor cell specific M2 isoform of pyruvate kinase.

Peking University Health Science Center
GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).

Genentech
Synthesis and biological activity of peptide proline-boronic acids as proteasome inhibitors.

Peking University
Synthesis and evaluation of hydroxychalcones as multifunctional non-purine xanthine oxidase inhibitors for the treatment of hyperuricemia.

Guangxi Medical University
A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.

Genentech
SPIROCYCLIC LACTAM INHIBITORS

Incyte
TRIAZINE DERIVATIVES FOR THE TREATMENT OF TUMOURS AND NEURODEGENERATIVE DISORDERS

UNIVERSITA'' DEGLI STUDI DI MILANO
Aryl sultam derivatives as RORc modulators

Genentech
Crystalline forms of a PI3K inhibitor

Incyte
Modulators of ATP-binding cassette transporters

Vertex Pharmaceuticals
Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists

Rugen Holdings (Cayman)
Aminopyrimidine derivatives as LRRK2 modulators

Genentech
Tyrosine kinase inhibitors. 2. Synthesis of 2,2'-dithiobis(1H-indole-3-alkanamides) and investigation of their inhibitory activity against epidermal growth factor receptor and pp60v-src protein tyrosine kinases.

University of Auckland
5-chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase.

Merck Research Laboratories