119 articles for J Guo
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Development of 2, 4-diaminoquinazoline derivatives as potent PAK4 inhibitors by the core refinement strategy.
Shenyang Pharmaceutical University
A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units.
Abbott Laboratories
Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.
Abbott Laboratories
A Cyclic Tetrapeptide ("Cyclodal") and Its Mirror-Image Isomer Are Both High-Affinityµ Opioid Receptor Antagonists.
Clinical Research Institute of Montreal
Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.
Vitae Pharmaceuticals
Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR)ß Agonist.
Vitae Pharmaceuticals
Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
Bristol-Myers Squibb Research and Development
Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).
Bristol-Myers Squibb Research and Development
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.
Bristol-Myers Squibb Research & Development
Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2.
Abbvie
Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.
Translational Research Institute
Discovery of novel 2,4-diarylaminopyrimidine analogues (DAAPalogues) showing potent inhibitory activities against both wild-type and mutant ALK kinases.
Chinese Academy of Sciences
Design, synthesis and pharmacological evaluation of 2-(thiazol-2-amino)-4-arylaminopyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Shanghai Institute of Materia Medica (Simm)
Discovery and development of potent and selective inhibitors of histone methyltransferase g9a.
Abbvie
Mono-carbonyl curcumin analogues as 11ß-hydroxysteroid dehydrogenase 1 inhibitors.
Wenzhou Medical College
Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-ß-alanine (MK-0893) for the treatment of type II diabetes.
Merck Research Laboratories
Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.
TBA
"Carba"-analogues of fentanyl are opioid receptor agonists.
Clinical Research Institute of Montreal
A docking score function for estimating ligand-protein interactions: application to acetylcholinesterase inhibition.
University of Kansas
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): synthesis and initial structure-activity relationships.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of N-[2-[2-[[3-methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a novel and potent inhibitor of inosine monophosphate dehydrogenase with excellent in vivo activity.
TBA
Synthesis and pharmacological evaluation of N-(2,5-disubstituted phenyl)-N'-(3-substituted phenyl)-N'-methylguanidines as N-methyl-D-aspartate receptor ion-channel blockers.
Cambridge Neuroscience
S-(5'-deoxy-5'-adenosyl)-1-aminoxy-4-(methylsulfonio)-2-cyclopentene (AdoMao): an irreversible inhibitor of S-adenosylmethionine decarboxylase with potent in vitro antitrypanosomal activity.
Wayne State University
Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library.
Pharmacopeia
Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1 (MLN0905).
Millennium Pharmaceuticals
Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).
Bristol-Myers Squibb Research and Development
Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11ß-hydroxysteroid dehydrogenase type 1.
Vitae Pharmaceuticals
Biphenyl/diphenyl ether renin inhibitors: filling the S1 pocket of renin via the S3 pocket.
Vitae Pharmaceuticals
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.
Bristol-Myers Squibb
Discovery and optimization of adamantyl carbamate inhibitors of 11ß-HSD1.
Vitae Pharmaceuticals
Spirocyclic ureas: orally bioavailable 11beta-HSD1 inhibitors identified by computer-aided drug design.
Vitae Pharmaceuticals
Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.
Bristol-Myers Squibb Research and Development
Identification of potent pyrimidine inhibitors of phosphodiesterase 7 (PDE7) and their ability to inhibit T cell proliferation.
Bristol-Myers Squibb Pharmaceutical Research Institute
Bornyl- and isobornyl-Delta8-tetrahydrocannabinols: a novel class of cannabinergic ligands.
Northeastern University
The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia.
Abbvie
Discovery of novel benzimidazole derivatives as selective and reversible monoamine oxidase B inhibitors for Parkinson's disease treatment.
Zhejiang University
Thiazole-based analogues as potential antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA) and their SAR elucidation.
Jiangxi Science & Technology Normal University
Conformationally constrained analogues of 2-arachidonoylglycerol.
Northeastern University
C1'-cycloalkyl side chain pharmacophore in tetrahydrocannabinols.
National Hellenic Research Foundation
Beyond inhibition against the PD-1/PD-L1 pathway: development of PD-L1 inhibitors targeting internalization and degradation of PD-L1.
China Pharmaceutical University
Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.
University of Michigan
Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.
University of Michigan
Discovery of novel benzbromarone analogs with improved pharmacokinetics and benign toxicity profiles as antihyperuricemic agents.
Southern Medical University
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.
Abbott Laboratories
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
Novel neuroprotective pyromeconic acid derivatives with concurrent anti-Aβ deposition, anti-inflammatory, and anti-oxidation properties for treatment of Alzheimer's disease.
Fujian Medical University
Discovery of AXL Degraders with Improved Potencies in Triple-Negative Breast Cancer (TNBC) Cells.
Jinan 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
Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.
University of Michigan
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.
Abbott Laboratories
Design, Synthesis, and Proof-of-Concept of Triple-Site Inhibitors against Aminoacyl-tRNA Synthetases.
Sun Yat-Sen University
Design, synthesis, and progress toward optimization of potent small molecule antagonists of CC chemokine receptor 8 (CCR8).
Millennium Pharmaceuticals
Discovery and radiosensitization research of ursolic acid derivatives as SENP1 inhibitors.
Peking Union Medical College
Discovery of Natural Ursane-type SENP1 Inhibitors and the Platinum Resistance Reversal Activity Against Human Ovarian Cancer Cells: A Structure-Activity Relationship Study.
Peking Union Medical College
Discovery of Isoform-Selective Akt3 Degraders Overcoming Osimertinib-Induced Resistance in Non-Small Cell Lung Cancer Cells.
Jinan University
Discovery of novel TrkA allosteric inhibitors: Structure-based virtual screening, biological evaluation and preliminary SAR studies.
Jinan University
Identification of purine inhibitors of phosphodiesterase 7 (PDE7).
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer.
Millennium Pharmaceuticals, A Wholly Owned Subsidiary of Takeda Pharmaceuticals
Pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable Threonine Tyrosine Kinase (TTK) inhibitors.
Guangzhou Institutes of Biomedicine and Health
Design, synthesis and biological evaluation of novel benzoxaborole derivatives as potent PDE4 inhibitors for topical treatment of atopic dermatitis.
China Pharmaceutical University
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
Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety.
Bristol-Myers Squibb Pharmaceutical Research Institute
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
Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues.
Bristol-Myers Squibb Pri
Novel inhibitors of IMPDH: a highly potent and selective quinolone-based series.
Bristol-Myers Squibb Pri
A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase.
Bristol-Myers Squibb Pharmaceutical Research Institute
The discovery of novel small molecule allosteric activators of aldehyde dehydrogenase 2.
Second Military Medical University
Rapid synthesis of triazine inhibitors of inosine monophosphate dehydrogenase.
Bristol-Myers Squibb Pharmaceutical Research Institute
Novel diamide-based inhibitors of IMPDH.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of bazedoxifene analogues targeting glycoprotein 130.
China Pharmaceutical University
Design, Synthesis, and Biological Evaluation of Linear Aliphatic Amine-Linked Triaryl Derivatives as Potent Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction with Promising Antitumor Effects In Vivo.
National Engineering Research Center For The Emergency Drug
Solution-phase, parallel synthesis and pharmacological evaluation of acylguanidine derivatives as potential sodium channel blockers.
Cenes Pharmaceuticals
Soluble guanylate cyclase stimulators for the treatment of hypertension: Discovery of MK-2947.
Merck
Rational design, synthesis and biological evaluation of novel multitargeting anti-AD iron chelators with potent MAO-B inhibitory and antioxidant activity.
Zhejiang University
Discovery of arylbenzylamines as PDE4 inhibitors with potential neuroprotective effect.
Southern Medical University
Synthesis and biological evaluation of 7-methoxy-1-(3,4,5-trimethoxyphenyl)-4,5-dihydro-2H-benzo[e]indazoles as new colchicine site inhibitors.
Second Military Medical University
Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage.
Bristol-Myers Squibb Research & Development
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.
Bristol-Myers Squibb
Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.
Universities of Shandong
Design, synthesis and biological evaluation of novel 7H-pyrrolo[2,3-d]pyrimidine derivatives as potential FAK inhibitors and anticancer agents.
Shenyang Pharmaceutical University
Transition State-Based Sialyltransferase Inhibitors: Mimicking Oxocarbenium Ion by Simple Amide.
Peking University
Novel tetracyclic benzo[b]carbazolones as highly potent and orally bioavailable ALK inhibitors: design, synthesis, and structure-activity relationship study.
Chinese Academy of Sciences
Development of novel β-carboline-based hydroxamate derivatives as HDAC inhibitors with antiproliferative and antimetastatic activities in human cancer cells.
Nantong University
Natural Product Micheliolide (MCL) Irreversibly Activates Pyruvate Kinase M2 and Suppresses Leukemia.
Nankai 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
Development of novel amino-quinoline-5,8-dione derivatives as NAD(P)H:quinone oxidoreductase 1 (NQO1) inhibitors with potent antiproliferative activities.
Nantong University
Discovery of highly potent, selective, covalent inhibitors of JAK3.
Bristol-Myers Squibb Research and Development
SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT).
Abbvie
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor.
Vitae Pharmaceuticals
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
COMPOSITION FOR PREVENTING OR TREATING GRAVES' DISEASE COMPRISING COMPOUND CONTAINING AN IMIDAZOPYRIDINE STRUCTURE AS ACTIVE INGREDIENT
Esgelbio
NAMPT ACTIVATORS FOR TREATING METABOLIC AND NEUROLOGICAL DISORDERS
University of Illinois
Methylamine derivatives as lysysl oxidase inhibitors for the treatment of cancer
The Institute of Cancer Research: Royal Cancer Hospital
Imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines as mark inhibitors
Merck Sharp & Dohme
Phytoestrogenic formulations for alleviation or prevention of neurodegenerative diseases
University of Southern California
Characterization of central- and peripheral-type benzodiazepine receptors in rat salivary glands.
Tokyo Dental College
Biochemical and pharmacological characterization of high-affinity trimetoquinol analogs on guinea pig and human beta adrenergic receptor subtypes: evidence for partial agonism.
Ohio State University
1-(m-chlorophenyl)piperazine (mCPP) interactions with neurotransmitter receptors in the human brain.
Stanford University
Development of a novel virtual screening cascade protocol to identify potential trypanothione reductase inhibitors.
University of Alberta
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.
Hoffmann-La Roche
Carbonic anhydrase and matrix metalloproteinase inhibitors: sulfonylated amino acid hydroxamates with MMP inhibitory properties act as efficient inhibitors of CA isozymes I, II, and IV, and N-hydroxysulfonamides inhibit both these zinc enzymes.
Universita Degli Studi