110 articles for X He
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
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Article Title
Organization
Acyl-2-aminobenzimidazoles: a novel class of neuroprotective agents targeting mGluR5.
University of Maryland
New coumarin derivatives: design, synthesis and use as inhibitors of hMAO.
Anhui Medical University
Novel carboline derivatives as potent antifungal lead compounds: design, synthesis, and biological evaluation.
Second Military Medical University
New 2H-chromene-3-carboxamide derivatives: design, synthesis and use as inhibitors of hMAO.
Anhui Medical University
Syk inhibitors with high potency in presence of blood.
Novartis Institutes For Biomedical Research
Design, synthesis and pharmacological evaluation of novel tacrine-caffeic acid hybrids as multi-targeted compounds against Alzheimer's disease.
Sun Yat-Sen University
Discovery and optimization of benzenesulfonanilide derivatives as a novel class of 11ß-HSD1 inhibitors.
Amgen
Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor.
Sun Yat-Sen University
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 1: Tuning the N-substituents.
Chinese Academy of Sciences
Optimization of novel di-substituted cyclohexylbenzamide derivatives as potent 11 beta-HSD1 inhibitors.
Amgen
Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model.
Amgen
Synthesis and evaluation of N-aryl pyrrolidinones as novel anti-HIV-1 agents. Part 1.
Genomics Institute of The Novartis Research Foundation
Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo.
Dupont Pharmaceuticals
Pharmacophore/receptor models for GABA(A)/BzR subtypes (alpha1beta3gamma2, alpha5beta3gamma2, and alpha6beta3gamma2) via a comprehensive ligand-mapping approach.
University of Wisconsin-Milwaukee
Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites.
National Institute of Diabetes and Digestive and Kidney Diseases
Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.
Institute of Pharmacology & Toxicology
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents.
Chinese Academy of Sciences
Potent matrix metalloproteinase inhibitors: Amino-carboxylate compounds containing modifications of the P1 residue
TBA
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1).
TBA
Distinctive molecular inhibition mechanisms for selective inhibitors of human 11beta-hydroxysteroid dehydrogenase type 1.
Amgen
Synthesis, cytotoxicity, antioxidant activity and molecular modeling of new NSAIDs-EBS derivatives.
Jianghan University
Design, synthesis and biological evaluation of indazole derivatives as selective covalent inhibitors of FGFR4 in wild-type and gatekeeper mutants.
Sichuan University
Recent advances of novel fourth generation EGFR inhibitors in overcoming C797S mutation of lung cancer therapy.
Hangzhou Normal University
Design, synthesis and antitumor activity of a novel FGFR2-selective degrader to overcome resistance of the FGFR2V564F gatekeeper mutation based on a pan-FGFR inhibitor.
Sichuan University
The discovery of novel and potent indazole NLRP3 inhibitors enabled by DNA-encoded library screening.
BioAge Labs
Design, synthesis, and biological evaluation of 4-(2-fluorophenoxy)-7-methoxyquinazoline derivatives as dual EGFR/c-Met inhibitors for the treatment of NSCLC.
Jiangxi Science & Technology Normal University
Medicinal chemistry strategies targeting NLRP3 inflammasome pathway: A recent update from 2019 to mid-2023.
Shenyang Pharmaceutical University
Design, Synthesis, and Biological Evaluation of 5-(5-Iodo-2-isopropyl-4-methoxyphenoxy)pyrimidine-2,4-diamine (AF-353) Derivatives as Novel DHFR Inhibitors against Staphylococcus aureus.
Sichuan University
Progress in the controllability technology of PROTAC.
Changzhou Vocational Institute of Engineering
Discovery of potent small molecule ubiquitin-specific protease 10 inhibitors with anti-hepatocellular carcinoma activity through regulating YAP expression.
Zhejiang University
Exploration of novel isoxazole-fused quinone derivatives as anti-colorectal cancer agents through inhibiting STAT3 and elevating ROS level.
Sichuan University
Facile Synthesis and First Antifungal Exploration of Tetracyclic Meroterpenoids: (+)-Aureol, (-)-Pelorol, and Its Analogs.
Guizhou University
Switch type I to type II TRK inhibitors for combating clinical resistance induced by xDFG mutation for cancer therapy.
Jinan University
Selective Covalent Targeting of Pyruvate Kinase M2 Using Arsenous Warheads.
Chinese Academy of Sciences
Design and Synthesis of 1,3,5-Triazines or Pyrimidines Containing Dithiocarbamate Moiety as PI3Kα Selective Inhibitors.
Shenyang Pharmaceutical University
Design, synthesis, and biological evaluation of novel dihydropteridone derivatives possessing oxadiazoles moiety as potent inhibitors of PLK1.
Shenyang Pharmaceutical University
Discovery of novel PDE4 inhibitors targeting the M-pocket from natural mangostanin with improved safety for the treatment of Inflammatory Bowel Diseases.
Guangzhou University of Chinese Medicine
Discovery and optimization of dihydropteridone derivatives as novel PLK1 and BRD4 dual inhibitor for the treatment of cancer.
Shenyang Pharmaceutical University
Discovery of a novel GPR35 agonist with high and equipotent species potency for oral treatment of IBD.
University of Chinese Academy of Sciences
A TNF-α blocking peptide that reduces NF-κB and MAPK activity for attenuating inflammation.
Changchun University of Science and Technology
Design and synthesis of boron-containing ALK inhibitor with favorable in vivo efficacy.
Nanjing University
Pyrazolone structural motif in medicinal chemistry: Retrospect and prospect.
Northwest University
A concise review of recent advances in anti-heart failure targets and its small molecules inhibitors in recent years.
University of Electronic Science and Technology of China
Computational methods-guided design of modulators targeting protein-protein interactions (PPIs).
Shanghai Jiao Tong University
Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).
Incyte Research Institute
Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2.
Genomics Institute of The Novartis Research Foundation
Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1.
Genomics Institute of The Novartis Research Foundation
Medicinal chemistry updates of novel HDACs inhibitors (2020 to present).
Hangzhou Normal University
Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.
Zhejiang University
Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present).
Hangzhou Normal University
The evolution paths of some reprehensive scaffolds of RORγt modulators, a perspective from medicinal chemistry.
Sun Yat-Sen University
Synthesis and biological evaluation of a tumor-selective degrader of PARP1.
West China Hospital of Sichuan University
Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.
Prelude Therapeutics
Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B.
Chinese Academy of Sciences
Discovery of the First Potent IDO1/IDO2 Dual Inhibitors: A Promising Strategy for Cancer Immunotherapy.
China Pharmaceutical University
Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors.
Bristol-Myers Squibb Pharmaceutical Research Institute
Structure-activity relationship investigation for imidazopyrazole-3-carboxamide derivatives as novel selective inhibitors of Bruton's tyrosine kinase.
Henan Normal University
Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors.
Sichuan University
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
Identification of novel potent bicyclic peptide deformylase inhibitors.
Genomics Institute of The Novartis Research Foundation
Mangostanin Derivatives as Novel and Orally Active Phosphodiesterase 4 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis with Improved Safety.
Hainan University
Discovery of potent and selective Bcl-2 inhibitors with acyl sulfonamide skeleton.
Shanghai Institute of Pharmaceutical Industry
Structure-Based Design of Selective LONP1 Inhibitors for Probing
Genomics Institute of The Novartis Research Foundation
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 2: lead optimization.
Bristol-Myers Squibb Pharmaceutical Research Institute
Rational design, synthesis and structure-activity relationships of a cyclic succinate series of TNF-alpha converting enzyme inhibitors. Part 1: lead identification.
Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of novel pyrazolopyrimidine derivatives as potent mTOR/HDAC bi-functional inhibitors via pharmacophore-merging strategy.
Anhui University of Chinese Medicine
Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Bristol-Myers Squibb Pharmaceutical Research Institute
Carvedilol serves as a novel CYP1B1 inhibitor, a systematic drug repurposing approach through structure-based virtual screening and experimental verification.
Shenyang Pharmaceutical University
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 2: asymmetric synthesis and biological evaluation.
Neurogen
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.
Neurogen
Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors.
Amgen
Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as α7 nicotinic receptor antagonists.
Peking University
Discovery of macrocyclic hydroxamic acids containing biphenylmethyl derivatives at P1', a series of selective TNF-alpha converting enzyme inhibitors with potent cellular activity in the inhibition of TNF-alpha release.
Dupont Pharmaceuticals
4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors.
Liaocheng University
Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors.
Chia Tai Tianqing Pharmaceutical Group
Synthesis and evaluation of 4-(1,3,4-oxadiazol-2-yl)-benzenesulfonamides as potent carbonic anhydrase inhibitors.
Northwest A&F University
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).
Incyte
Discovery of fused heterocyclic carboxamide derivatives as novel α7-nAChR agonists: Synthesis, preliminary SAR and biological evaluation.
Peking University
Allosteric Modulator Discovery: From Serendipity to Structure-Based Design.
Shanghai Jiao-Tong University School of Medicine
Discovery and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.
Guangzhou University of Chinese Medicine
Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.
Northwest University
Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines at five recombinant GABAA/benzodiazepine receptor subtypes [alphaxbeta3gamma2 (x = 1-3, 5, and 6)] via comparative molecular field analysis.
University of Wisconsin-Milwaukee
Design and synthesis of cyclic inhibitors of matrix metalloproteinases and TNF-alpha production.
Dupont Pharmaceuticals
Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
Northwest University
Synthesis, structure-activity relationship and biological evaluation of novel arylpiperzines as α1A/1D-AR subselective antagonists for BPH.
Jinan University
Discovery of novel, potent and low-toxicity angiotensin II receptor type 1 (AT1) blockers: Design, synthesis and biological evaluation of 6-substituted aminocarbonyl benzimidazoles with a chiral center.
Beijing Institute of Technology
Design and synthesis of novel β-diketo derivatives as HIV-1 integrase inhibitors.
Beijing University of Technology
Discovery of N-aryl-N'-pyrimidin-4-yl ureas as irreversible L858R/T790M mutant selective epidermal growth factor receptor inhibitors.
Shanghai Haiyan Pharmaceutical Technology Co. Itd.
Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines.
Shanghai Haiyan Pharmaceutical Technology
Design, synthesis and anticancer activities evaluation of novel 5H-dibenzo[b,e]azepine-6,11-dione derivatives containing 1,3,4-oxadiazole units.
China Medical University
Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases.
Genomics Institute of The Novartis Research Foundation
Discovery of pentacyclic triterpene 3β-ester derivatives as a new class of cholesterol ester transfer protein inhibitors.
China Pharmaceutical University
TREATMENT OF MYELOPROLIFERATIVE DISEASES AND DISORDERS WITH INHIBITORS OF BET FAMILY BDII BROMODOMAIN
Poseidon Innovation 1
Discovery of potent anilide inhibitors against the severe acute respiratory syndrome 3CL protease.
National Taiwan University
Evaluation of short-tether bis-THA AChE inhibitors. A further test of the dual binding site hypothesis.
Hong Kong University of Science and Technology