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Development of 2, 4-diaminoquinazoline derivatives as potent PAK4 inhibitors by the core refinement strategy.

Shenyang Pharmaceutical University
Discovery of biphenyl imidazole derivatives as potent antifungal agents: Design, synthesis, and structure-activity relationship studies.

Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel cholesteryl ester transfer protein inhibitors bearing a cycloalkene scaffold.

Shenyang Pharmaceutical University
Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK).

Teva Branded Pharmaceutical Products R & D
Design, synthesis and biological evaluation of N,N-3-phenyl-3-benzylaminopropanamide derivatives as novel cholesteryl ester transfer protein inhibitor.

Shenyang Pharmaceutical University
Discovery of novel N,N-3-phenyl-3-benzylaminopropionanilides as potent inhibitors of cholesteryl ester transfer protein in vivo.

Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel 4-phenoxy-6,7-disubstituted quinolines possessing (thio)semicarbazones as c-Met kinase inhibitors.

Shenyang Pharmaceutical University
Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.

Teva Branded Pharmaceutical Products R & D
Synthesis and biological evaluation of 3-phenyl-3-aryl carboxamido propanoic acid derivatives as small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26A1).

Key Laboratory of Structure-Based Drug Design and Discovery (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)
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
Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.

Cephalon
Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.

Cephalon
Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.

TBA
Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.

Cephalon
Design, synthesis, and structure-activity relationships of novel insulin receptor tyrosine kinase activators.

Telik
Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors.

Kyoto Pharmaceutical University
Design, synthesis, and anaplastic lymphoma kinase (ALK) inhibitory activity for a novel series of 2,4,8,22-tetraazatetracyclo[14.3.1.1³,¿?¿.1¿?¿,¹³]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles.

Cephalon
Pyrazolone-based anaplastic lymphoma kinase (ALK) inhibitors: control of selectivity by a benzyloxy group.

Cephalon
2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazines: new variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity.

Cephalon
Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.

Cephalon
Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.

Cephalon
Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties.

Kyoto Pharmaceutical University
Discovery of novel indazole derivatives as second-generation TRK inhibitors.

Shenyang Pharmaceutical University
Design, synthesis, pharmacological evaluation, and computational study of benzo[d] isothiazol-based small molecule inhibitors targeting PD-1/PD-l1 interaction.

Shenyang Pharmaceutical University
The U.S. FDA approved cardiovascular drugs from 2011 to 2023: A medicinal chemistry perspective.

Sichuan University
Discovery of novel 3-(1H-pyrazol-4-yl)-1H-indazole derivatives as potent type II TRK inhibitors against acquired resistance.

Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of carbamate derivatives incorporating multifunctional carrier scaffolds as pseudo-irreversible cholinesterase inhibitors for the treatment of Alzheimer's disease.

Shenyang Pharmaceutical University
Identification of a Novel Selective CDK9 Inhibitor for the Treatment of CRC: Design, Synthesis, and Biological Activity Evaluation.

Shenyang Pharmaceutical University
Discovery of CZS-241: A Potent, Selective, and Orally Available Polo-Like Kinase 4 Inhibitor for the Treatment of Chronic Myeloid Leukemia.

Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel indolin-2-one derivatives as potent second-generation TRKs inhibitors.

Shenyang Pharmaceutical University
Identification of novel indole derivatives as highly potent and efficacious LSD1 inhibitors.

Shenyang Pharmaceutical University
A multi-target directed ligands strategy for the treatment of Alzheimer's disease: Dimethyl fumarate plus Tranilast modified Dithiocarbate as AChE inhibitor and Nrf2 activator.

Jiangxi University of Chinese Medicine
Discovery of the First Potent, Selective, and

Shenyang Pharmaceutical University
Structure-based discovery of 1-(3-fluoro-5-(5-(3-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-b]pyridin-3-yl)phenyl)-3-(pyrimidin-5-yl)urea as a potent and selective nanomolar type-II PLK4 inhibitor.

Shenyang Pharmaceutical University
Design, synthesis, and biological evaluation of diaminopyrimidine derivatives as novel focal adhesion kinase inhibitors.

Shenyang Pharmaceutical University
Discovery of novel dual Bruton's tyrosine kinase (BTK) and Janus kinase 3 (JAK3) inhibitors as a promising strategy for rheumatoid arthritis.

China Pharmaceutical University
Design, synthesis, and biological evaluation of novel pyrimidin-2-amine derivatives as potent PLK4 inhibitors.

Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of pyrazolo[3,4-

Shenyang Pharmaceutical University
Identification and in silicon binding study of a novel NR2B selective NMDAR antagonist.

Shenyang Pharmaceutical University
Dual functional antioxidant and butyrylcholinesterase inhibitors for the treatment of Alzheimer's disease: Design, synthesis and evaluation of novel melatonin-alkylbenzylamine hybrids.

Jiangxi University of Chinese Medicine
Discovery of a Highly Selective β

Shenyang Pharmaceutical University
Species-Selective Targeting of Fungal Hsp90: Design, Synthesis, and Evaluation of Novel 4,5-Diarylisoxazole Derivatives for the Combination Treatment of Azole-Resistant Candidiasis.

Shenyang Pharmaceutical University
Design, synthesis, and evaluation of novel 3-thiophene derivatives as potent fungistatic and fungicidal reagents based on a conformational restriction strategy.

Shenyang Pharmaceutical University
Rational drug design to explore the structure-activity relationship (SAR) of TRK inhibitors with 2,4-diaminopyrimidine scaffold.

Shenyang Pharmaceutical University
Discovery of quinazoline derivatives CZw-124 as a pan-TRK inhibitor with potent anticancer effects in vitro and in vivo.

Shenyang Pharmaceutical University
Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras.

Icahn School of Medicine At Mount Sinai
Identification of novel and potent PROTACs targeting FAK for non-small cell lung cancer: Design, synthesis, and biological study.

Shenyang Pharmaceutical University
Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.

Shenyang Pharmaceutical University
Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents.

Shenyang Pharmaceutical University
Identification and In Silico Binding Study of a Highly Potent DENV NS2B-NS3 Covalent Inhibitor.

Shenyang Pharmaceutical University
Improving the metabolic stability of antifungal compounds based on a scaffold hopping strategy: Design, synthesis, and structure-activity relationship studies of dihydrooxazole derivatives.

Shenyang Pharmaceutical University
8-Hydroxyquinolin-2(1H)-one analogues as potential β

Shenyang Pharmaceutical University
Design, synthesis, biological evaluation and pharmacophore model analysis of novel tetrahydropyrrolo[3,4-c]pyrazol derivatives as potential TRKs inhibitors.

Shenyang Pharmaceutical University
Structure-Based Discovery of Proline-Derived Arginase Inhibitors with Improved Oral Bioavailability for Immuno-Oncology.

Quantitative Biosciences
Design, synthesis and evaluation of novel 5-phenylthiophene derivatives as potent fungicidal of Candida albicans and antifungal reagents of fluconazole-resistant fungi.

Shenyang Pharmaceutical University
Utilization of Metabolite Identification and Structural Data to Guide Design of Low-Dose IDO1 Inhibitors.

Merck
Design, synthesis and biological evaluation of novel benzofuran derivatives as potent LSD1 inhibitors.

Shenyang Pharmaceutical University
SAR towards indoline and 3-azaindoline classes of IDO1 inhibitors.

Merck
Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-β aggregation against Alzheimer's disease.

Affiated Tumor Hospital of Guangxi Medical University
Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors.

Shenyang Pharmaceutical University
Synthesis, bioconversion, pharmacokinetic and pharmacodynamic evaluation of N-isopropyl-oxy-carbonyloxymethyl prodrugs of CZh-226, a potent and selective PAK4 inhibitor.

Shenyang Pharmaceutical University
Design, synthesis, and biological evaluation of novel xanthone-alkylbenzylamine hybrids as multifunctional agents for the treatment of Alzheimer's disease.

Jiangxi University of Traditional Chinese Medicine
Carbamate and

Merck
Design, synthesis and biological evaluation of tetrahydroquinoline-based reversible LSD1 inhibitors.

Shenyang Pharmaceutical University
Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors.

Merck
Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β

Shenyang Pharmaceutical University
Discovery and Optimization of Rationally Designed Bicyclic Inhibitors of Human Arginase to Enhance Cancer Immunotherapy.

Merck
Strategic Incorporation of Polarity in Heme-Displacing Inhibitors of Indoleamine-2,3-dioxygenase-1 (IDO1).

Merck
Design, synthesis and evaluation of biphenyl imidazole analogues as potent antifungal agents.

Shenyang Pharmaceutical University
Design and synthesis of piperazine-based matrix metalloproteinase inhibitors.

Procter and Gamble Pharmaceuticals
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.

Merck
Design, synthesis, and biological evaluation of matrix metalloproteinase inhibitors derived from a modified proline scaffold.

University of Florida
Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.

Icahn School of Medicine At Mount Sinai
Design and synthesis of conformationally-constrained MMP inhibitors.

Procter and Gamble Pharmaceuticals
Design, synthesis and biological evaluation of 5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one derivatives as potent β

Shenyang Pharmaceutical University
Discovery of Orally Bioavailable and Liver-Targeted Hypoxia-Inducible Factor Prolyl Hydroxylase (HIF-PHD) Inhibitors for the Treatment of Anemia.

Merck
Design, synthesis and biological evaluation of curcumin analogues as novel LSD1 inhibitors.

Shenyang Pharmaceutical University
Design, synthesis and biological evaluation of novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potential FAK inhibitors and anticancer agents.

Shenyang Pharmaceutical University
PB-10, a thiazolo[4,5-d] pyrimidine derivative, targets p21-activated kinase 4 in human colorectal cancer cells.

Inner Mongolia Medical University
Bridged gamma-carbolines and derivatives possessing selective and combined affinity for 5-HT2 and D2 receptors.

Scios Nova
Locking the two ends of tetrapeptidic HTLV-I protease inhibitors inside the enzyme.

Kyoto Pharmaceutical University
Synthesis and biological evaluation of β

Shenyang Pharmaceutical University
Synthesis and biological evaluation of NH

Shenyang Pharmaceutical University
Design, synthesis and evaluation of benzoheterocycle analogues as potent antifungal agents targeting CYP51.

Shenyang Pharmaceutical University
Identification of caffeoylquinic acid derivatives as natural protein tyrosine phosphatase 1B inhibitors from Artemisia princeps.

China Pharmaceutical University
Design, synthesis, structure-activity relationships study and X-ray crystallography of 3-substituted-indolin-2-one-5-carboxamide derivatives as PAK4 inhibitors.

Shenyang Pharmaceutical University
Design, synthesis and evaluation of aromatic heterocyclic derivatives as potent antifungal agents.

Shenyang Pharmaceutical University
Preparation of 5'-deoxy-5'-amino-5'-C-methyl adenosine derivatives and their activity against DOT1L.

Shenyang Pharmaceutical University
SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT).

Abbvie
Discovery of indolin-2-one derivatives as potent PAK4 inhibitors: Structure-activity relationship analysis, biological evaluation and molecular docking study.

Shenyang Pharmaceutical University
Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors.

Shenyang Pharmaceutical University
Inhibition studies of porphobilinogen synthase from Escherichia coli differentiating between the two recognition sites.

University of NeuchÂTel