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Discovery of Antimalarial Azetidine-2-carbonitriles That Inhibit

Harvard University
Design and synthesis of potent substrate-based inhibitors of the Trypanosoma cruzi dihydroorotate dehydrogenase.

Nagasaki University
Development of ML390: A Human DHODH Inhibitor That Induces Differentiation in Acute Myeloid Leukemia.

Broad Institute
Design, synthesis and inhibitory activity against human dihydroorotate dehydrogenase (hDHODH) of 1,3-benzoazole derivatives bearing amide units.

East China University of Science and Technology
Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH.

University of Malaya
Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH).

Institut Pasteur
Design, synthesis, X-ray crystallographic analysis, and biological evaluation of thiazole derivatives as potent and selective inhibitors of human dihydroorotate dehydrogenase.

East China University of Science and Techology
Original 2-(3-alkoxy-1H-pyrazol-1-yl)pyrimidine derivatives as inhibitors of human dihydroorotate dehydrogenase (DHODH).

Institut Pasteur
Design, synthesis and pharmacological evaluation of novel substituted quinoline-2-carboxamide derivatives as human dihydroorotate dehydrogenase (hDHODH) inhibitors and anticancer agents.

Nirma University
Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors.

University of Texas At Dallas
Novel selective and potent inhibitors of malaria parasite dihydroorotate dehydrogenase: discovery and optimization of dihydrothiophenone derivatives.

State Key Laboratory of Bioreactor Engineering
SAR Based Optimization of a 4-Quinoline Carboxylic Acid Analog with Potent Anti-Viral Activity.

University of Texas Southwestern Medical Center
On dihydroorotate dehydrogenases and their inhibitors and uses.

Institut Pasteur
Discovery of diverse human dihydroorotate dehydrogenase inhibitors as immunosuppressive agents by structure-based virtual screening.

State Key Laboratory of Bioreactor Engineering
Factors influencing the specificity of inhibitor binding to the human and malaria parasite dihydroorotate dehydrogenases.

University of Leeds
Bioisosteric transformations and permutations in the triazolopyrimidine scaffold to identify the minimum pharmacophore required for inhibitory activity against Plasmodium falciparum dihydroorotate dehydrogenase.

University of Washington
Lead optimization of 3-carboxyl-4(1H)-quinolones to deliver orally bioavailable antimalarials.

St. Jude Children'S Research Hospital
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.

Duquesne University
Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria.

TBA
Type II NADH dehydrogenase of the respiratory chain of Plasmodium falciparum and its inhibitors.

Harvard School of Public Health
Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists.

Wyeth Research
New dermatological agents for the treatment of psoriasis.

Allergan
Pyrazole bioisosteres of leflunomide as B-cell immunosuppressants for xenotransplantation and chronic rejection: scope and limitations.

Novartis Pharma
Synthesis, structure-activity relationships, and pharmacokinetic properties of dihydroorotate dehydrogenase inhibitors: 2-cyano-3-cyclopropyl-3-hydroxy-N-[3'-methyl-4'-(trifluoromethyl)phenyl ] propenamide and related compounds.

Hoechst Marion Roussel
Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.

Astrazeneca
Structure-guided lead optimization of triazolopyrimidine-ring substituents identifies potent Plasmodium falciparum dihydroorotate dehydrogenase inhibitors with clinical candidate potential.

Glaxosmithkline
New inhibitors of dihydroorotate dehydrogenase (DHODH) based on the 4-hydroxy-1,2,5-oxadiazol-3-yl (hydroxyfurazanyl) scaffold.

University of Turin
Biaryl analogues of teriflunomide as potent DHODH inhibitors.

RhôNe-Poulenc Rorer
Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.

University of Washington
1,2,5-Oxadiazole analogues of leflunomide and related compounds.

University of Turin
Discovery of novel inhibitors for DHODH via virtual screening and X-ray crystallographic structures.

Sanofi-Aventis
Immunosuppressive structure-activity relationships of Brequinar and related cinchoninic acid derivatives

TBA
Discovery and Optimization of Novel

Sichuan University
Development of a Potent Nurr1 Agonist Tool for In Vivo Applications.

Ludwig Maximilian University of Munich
Novel Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia.

Smith, Gambrell & Russell
Novel Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia.

Smith, Gambrell & Russell
Discovery of potent human dihydroorotate dehydrogenase inhibitors based on a benzophenone scaffold.

Sichuan University
Discovery of Alternative Binding Poses through Fragment-Based Identification of DHODH Inhibitors.

Janssen Pharmaceutical Research and Development
Basic Nitrogen (BaN) Is a Key Property of Antimalarial Chemical Space.

Birla Institute of Technology and Science Pilani
SAR studies toward discovery of emvododstat (PTC299), a potent dihydroorotate dehydrogenase (DHODH) inhibitor.

Ptc USA
Furazans in Medicinal Chemistry.

Treventis
Anticancer fungal natural products: Mechanisms of action and biosynthesis.

Sun Yat-Sen University
Enzyme inhibition potency enhancement by active site metal chelating and hydrogen bonding induced conformation-restricted cyclopropanecarbonyl derivatives.

Tunghai University
-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia.

Janssen Research and Development
A novel series of teriflunomide derivatives as orally active inhibitors of human dihydroorotate dehydrogenase for the treatment of colorectal carcinoma.

Sichuan University
Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.

West China Hospital
VHL-based PROTACs as potential therapeutic agents: Recent progress and perspectives.

The Affiliated Hospital of Qingdao University
Indazole and Benzoisoxazole Compounds as Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia.

Smith, Gambrell & Russell
SAR, species specificity, and cellular activity of cyclopentene dicarboxylic acid amides as DHODH inhibitors.

4Sc
Recent advances of human dihydroorotate dehydrogenase inhibitors for cancer therapy: Current development and future perspectives.

West China Hospital
Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-

University of Turin
An insight into the recent development of the clinical candidates for the treatment of malaria and their target proteins.

Jamia Millia Islamia (A Central University)
Design, Synthesis, and Biological Evaluation of a Novel Series of Teriflunomide Derivatives as Potent Human Dihydroorotate Dehydrogenase Inhibitors for Malignancy Treatment.

Sichuan University
Targeting Acute Myelogenous Leukemia Using Potent Human Dihydroorotate Dehydrogenase Inhibitors Based on the 2-Hydroxypyrazolo[1,5-

University of Turin
Discovery of Orally Available Retinoic Acid Receptor-Related Orphan Receptor γ-t/Dihydroorotate Dehydrogenase Dual Inhibitors for the Treatment of Refractory Inflammatory Bowel Disease.

Fudan University
Biaryl Compounds as Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia (AML).

Smith, Gambrell & Russell
Targeting Chikungunya Virus Replication by Benzoannulene Inhibitors.

Southern Research
Heterocyclic Compounds as Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia (AML).

Smith, Gambrell & Russell
Exploring Marine-Derived Ascochlorins as Novel Human Dihydroorotate Dehydrogenase Inhibitors for Treatment of Triple-Negative Breast Cancer.

Guangxi University of Chinese Medicine
Discovery of a novel series of DHODH inhibitors by a docking procedure and QSAR refinement.

4Sc
Low cytotoxic quinoline-4-carboxylic acids derived from vanillin precursors as potential human dihydroorotate dehydrogenase inhibitors.

University of Kragujevac
Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.

Medicines For Malaria Venture
Use of Dihydroorotate Dehydrogenase Inhibitors for Treatment of Autoimmune Diseases and Cancer.

Therachem Research Medilab
N-phenyl ureidobenzenesulfonates, a novel class of promising human dihydroorotate dehydrogenase inhibitors.

Laval University
Parallel synthesis of potent, pyrazole-based inhibitors of Helicobacter pylori dihydroorotate dehydrogenase.

Bristol-Myers Squibb
Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity.

University of Washington
A carboxylic acid isostere screen of the DHODH inhibitor Brequinar.

Janssen Pharmaceutical Research & Development
Cerpegin-derived furo[3,4-c]pyridine-3,4(1H,5H)-diones enhance cellular response to interferons by de novo pyrimidine biosynthesis inhibition.

Paris Descartes University
Dihydroorotate Dehydrogenase Inhibitors for Treating Acute Myelogenous Leukemia (AML).

Smith, Gambrell & Russell
Bifunctional Naphtho[2,3-

Sichuan University
Optimization of Tetrahydroindazoles as Inhibitors of Human Dihydroorotate Dehydrogenase and Evaluation of Their Activity and In Vitro Metabolic Stability.

Karolinska Institutet
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.

University of Washington
1,2,4-Triazolo[1,5-a]pyrimidines in drug design.

University of California
Synthesis of 2-,4,-6-, and/or 7-substituted quinoline derivatives as human dihydroorotate dehydrogenase (hDHODH) inhibitors and anticancer agents: 3D QSAR-assisted design.

Nirma University
Dihydroorotate dehydrogenase inhibitors in anti-infective drug research.

University of Turin (Unito)
Ligand-based design, synthesis and biochemical evaluation of potent and selective inhibitors of Schistosoma mansoni dihydroorotate dehydrogenase.

Universidade De S£O Paulo
1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview.

Chinese Academy of Sciences
The Development Process for Discovery and Clinical Advancement of Modern Antimalarials.

The Walter and Eliza Hall Institute of Medical Research
Isoxazolylthioamides as potential immunosuppressants a combinatorial chemistry approach.

Novartis Pharma
Heteroatom- and carbon-linked biphenyl analogs of Brequinar as immunosuppressive agents.

Dupont Pharmaceuticals
Structure-activity relationships (SAR) of some tetracyclic heterocycles related to the immunosuppressive agent Brequinar Sodium.

Dupont Pharmaceuticals
Hydroxyazole scaffold-based Plasmodium falciparum dihydroorotate dehydrogenase inhibitors: Synthesis, biological evaluation and X-ray structural studies.

University of Turin
Design, Synthesis, and Biological Evaluation of 4-Quinoline Carboxylic Acids as Inhibitors of Dihydroorotate Dehydrogenase.

University of Michigan
Targeting Myeloid Differentiation Using Potent 2-Hydroxypyrazolo[1,5- a]pyridine Scaffold-Based Human Dihydroorotate Dehydrogenase Inhibitors.

University of Turin
Interconvertible geometric isomers of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors exhibit multiple binding modes.

University of Leeds
INDAZOLE COMPOUND AND PHARMACEUTICAL

Nippon Shinyaku
In-flow photooxygenation of aminothienopyridinones generates PTP4A3 phosphatase inhibitors

University of Virginia Patent Foundation
OXAZEPINE COMPOUNDS AND USES THEREOF IN THE TREATMENT OF CANCER

Genentech
ANNULATED 2-AMINO-3-CYANO THIOPHENES AND DERIVATIVES FOR THE TREATMENT OF CANCER

Boehringer Ingelheim International
BET SUBFAMILY INHIBITORS AND METHODS USING SAME

Baylor College of Medicine
INHIBITORS OF CYSTEINE PROTEASES

Texas A&M University
COMPOUNDS FOR THE TREATMENT OF SARS

Purdue Research Foundation
SALT INDUCIBLE KINASE INHIBITORS

The General Hospital
Thiadiazole IRAK4 inhibitors

Gilead Sciences
N-(substituted-phenyl)-sulfonamide derivatives as kinase inhibitors

Nerviano Medical Sciences
Aminopyrimidinyl compounds

Pfizer
Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators

Janssen Pharmaceutica
Substituted 1,6-dihydropyridinones and 1,2-dihydroisoquinolinones as bet inhibitors

Nuvation Bio
Compositions for APP-selective BACE inhibition and uses therefor

University of California
Pyrrolo-pyridine derivative compound, method for preparing same, and pharmaceutical composition containing same as active ingredient for prevention or treatment of protein kinase-related diseases

TBA
Cycloalkyl substituted triazole compounds as agonists of the APJ receptor

Amgen
Chemical compounds

Astrazeneca
Benzene disulfonamide for the treatment of cancer

Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften
Bruton's tyrosine kinase inhibitors

Suzhou Baijibugong Pharmaceutical Technology
WDR5-MLL1 inhibitors and modulators

Vanderbilt University
Geminal substituted quinuclidine amide compounds as agonists of α-7 nicotonic acetylcholine receptors

Axovant Sciences
Autotaxin inhibitors

Novartis
Indolizine compounds, a process for their preparation and pharmaceutical compositions containing them

Les Laboratoires Servier
Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof

Shanghai Yingli Pharmaceutical
Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use

Genentech
Spiro-thiazolones

Hoffmann-La Roche
Necrosis inhibitors

National Institute of Biological Sciences, Beijing
Aglaroxin C and derivatives as HCV entry inhibitors

Sri International
RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.

Roche Bioscience
Characterization of human recombinant neuronal nicotinic acetylcholine receptor subunit combinations alpha2beta4, alpha3beta4 and alpha4beta4 stably expressed in HEK293 cells.

Sibia Neurosciences
D4 dopamine receptor binding affinity does not distinguish between typical and atypical antipsychotic drugs.

Case Western Reserve University
Fluorescence polarization assay and inhibitor design for MDM2/p53 interaction.

Schering-Plough Research Institute
Isoindolinone ureas: a novel class of KDR kinase inhibitors.

Abbott Laboratories