161 articles for thisTarget
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Synthesis and evaluation of 5-(1H-indol-3-yl)-N-aryl-1,3,4-oxadiazol-2-amines as Bcl-2 inhibitory anticancer agents.
Cardiff University
Design, synthesis and preliminary biological evaluation of indole-3-carboxylic acid-based skeleton of Bcl-2/Mcl-1 dual inhibitors.
Shandong University
Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains.
Shandong University
Gossypol with Hydrophobic Linear Esters Exhibits Enhanced Antitumor Activity as an Inhibitor of Antiapoptotic Proteins.
Wuhan University School of Pharmaceutical Sciences
Design, synthesis, and activity evaluation of selective inhibitors of anti-apoptotic Bcl-2 proteins: The effects on the selectivity of the P1 pockets in the active sites.
China Pharmaceutical University
Structural modification of luteolin from Flos Chrysanthemi leads to increased tumor cell growth inhibitory activity.
Second Military Medical University
Selective inhibitors of Bcl-2 and Bcl-xL: Balancing antitumor activity with on-target toxicity.
Astrazeneca
Design, synthesis and preliminary bioactivity studies of imidazolidine-2,4-dione derivatives as Bcl-2 inhibitors.
Shandong University
Design, synthesis and biological evaluation of 3-aryl-rhodanine benzoic acids as anti-apoptotic protein Bcl-2 inhibitors.
Shandong University
Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.
Novartis Institutes For Biomedical Research
Discovery of tricyclic indoles that potently inhibit Mcl-1 using fragment-based methods and structure-based design.
Vanderbilt University School of Medicine
Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.
Abbvie
Structure-based lead optimization and biological evaluation of BAX direct activators as novel potential anticancer agents.
University of Naples Federico II
Design, synthesis and preliminary bioactivity studies of 2-thioxo-4-thiazolidinone derivatives as Bcl-2 inhibitors.
Shandong University
In vitro induction of apoptosis by isosclerone from marine-derived fungus Aspergillus fumigatus.
Pukyong National University
3-Substituted-N-(4-hydroxynaphthalen-1-yl)arylsulfonamides as a novel class of selective Mcl-1 inhibitors: structure-based design, synthesis, SAR, and biological evaluation.
University of Michigan Medical School
Design and application of a rigid quinazolone scaffold based on two-face Bima-helix mimicking.
Dalian University of Technology
Discovery of potent and selective benzothiazole hydrazone inhibitors of Bcl-XL.
The Walter and Eliza Hall Institute of Medical Research
Synthesis and evaluation of 3-(benzylthio)-5-(1H-indol-3-yl)-1,2,4-triazol-4-amines as Bcl-2 inhibitory anticancer agents.
Cardiff University
The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions.
Novartis Institutes For Biomedical Research
Fragment-based design, synthesis, and biological evaluation of N-substituted-5-(4-isopropylthiophenol)-2-hydroxynicotinamide derivatives as novel Mcl-1 inhibitors.
Dalian University of Technology
Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design.
Vanderbilt University School of Medicine
3-Thiomorpholin-8-oxo-8H-acenaphtho [1,2-b] pyrrole-9-carbonitrile (S1) derivatives as pan-Bcl-2-inhibitors of Bcl-2, Bcl-xL and Mcl-1.
Dalian University of Technology
Synopsis of some recent tactical application of bioisosteres in drug design.
Bristol-Myers Squibb Pharmaceutical Research and Development
An anthraquinone scaffold for putative, two-face Bim BH3a-helix mimic.
Dalian University of Technology
Synthesis and biological activities of polyquinoline derivatives: new Bcl-2 family protein modulators.
Clermont Universit£
Structure-based discovery of BM-957 as a potent small-molecule inhibitor of Bcl-2 and Bcl-xL capable of achieving complete tumor regression.
University of Michigan
Design of Bcl-2 and Bcl-xL inhibitors with subnanomolar binding affinities based upon a new scaffold.
University of Michigan
Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists.
Bristol-Myers Squibb Research
Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists.
Bristol-Myers Squibb Research
BI-97C1, an optically pure Apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
Sanford-Burnham Medical Research Institute
Development of dimeric modulators for anti-apoptotic Bcl-2 proteins.
University of Minnesota Minneapolis
Development of selective inhibitors for anti-apoptotic Bcl-2 proteins from BHI-1.
University of Minnesota
Discovery of small-molecule inhibitors of Bcl-2 through structure-based computer screening.
Georgetown University Medical Center
Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: characteristics of broad-spectrum protein binding and its effects on anti-tumor activity.
Second Military Medical University
Probing the difference between BH3 groove of Mcl-1 and Bcl-2 protein: Implications for dual inhibitors design.
Dalian University of Technology
Quinazoline sulfonamides as dual binders of the proteins B-cell lymphoma 2 and B-cell lymphoma extra long with potent proapoptotic cell-based activity.
The Walter and Eliza Hall Institute of Medical Research
3-Thiomorpholin-8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile (S1) based molecules as potent, dual inhibitors of B-cell lymphoma 2 (Bcl-2) and myeloid cell leukemia sequence 1 (Mcl-1): structure-based design and structure-activity relationship studies.
Dalian University of Technology
Synthesis and biological evaluation of Apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.
Sanford-Burnham Medical Research Institute
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
Aristotle University of Thessaloniki
Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.
Abbott Laboratories
Design, synthesis, and interaction study of quinazoline-2(1H)-thione derivatives as novel potential Bcl-xL inhibitors.
Chinese Academy of Sciences
Vaccinia virus virulence factor N1L is a novel promising target for antiviral therapeutic intervention.
Institute For Medical Research
Diversity-oriented synthesis of a cytisine-inspired pyridone library leading to the discovery of novel inhibitors of Bcl-2.
Infinity Pharmaceuticals
Atropisomeric small molecule Bcl-2 ligands: determination of bioactive conformation.
Ucb Pharma
Tetrahydroisoquinoline amide substituted phenyl pyrazoles as selective Bcl-2 inhibitors.
Ucb Pharma
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.
Abbott Laboratories
Structure-activity relationships of Bak derived peptides: affinity and specificity modulations by amino acid replacement.
University of Montpellier
Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.
University of Michigan
Targeting the Inhibition of B-Cell Lymphoma 2 Protein for the Treatment of Cancer.
Therachem Research Medilab
Pyrogallol-based molecules as potent inhibitors of the antiapoptotic Bcl-2 proteins.
University of Michigan
Discovery and optimization of (2-naphthylthio)acetic acid derivative as selective Bfl-1 inhibitor.
Tianjin University
A decade of approved first-in-class small molecule orphan drugs: Achievements, challenges and perspectives.
China Pharmaceutical University
PROTAC: Harnessing Targeted Chimeras for Selective BCL-2 Degradation in Cancer Treatment.
Usona Institute
Structure-activity relationship studies of ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (HA 14-1), an antagonist for antiapoptotic Bcl-2 proteins to overcome drug resistance in cancer.
University of Minnesota
Sulfonamide derivatives as potential anti-cancer agents and their SARs elucidation.
Hunan University of Science and Technology
Inhibitors of BCL2A1/Bfl-1 protein: Potential stock in cancer therapy.
China Pharmaceutical University
Single and dual target inhibitors based on Bcl-2: Promising anti-tumor agents for cancer therapy.
Shandong First Medical University & Shandong Academy of Medical Sciences
Structure-based design of potent small-molecule inhibitors of anti-apoptotic Bcl-2 proteins.
University of Michigan
Recent contributions of quinolines to antimalarial and anticancer drug discovery research.
Ghent University
Molecular hybrids: A five-year survey on structures of multiple targeted hybrids of protein kinase inhibitors for cancer therapy.
Al-Azhar University
Discovery of a selective and covalent small-molecule inhibitor of BFL-1 protein that induces robust apoptosis in cancer cells.
Yancheng Teachers University
Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.
Abbott Laboratories
Structural insights of oxindole based kinase inhibitors as anticancer agents: Recent advances.
National Institute of Pharmaceutical Education and Research (NIPER)
Novel Bcl-2 Inhibitors Selectively Disrupt the Autophagy-Specific Bcl-2-Beclin 1 Protein-Protein Interaction.
University of Texas Southwestern Medical Center
A chemical strategy to promote helical peptide-protein interactions involved in apoptosis.
University of Illinois At Urbana-Champaign
Development of Mcl-1 inhibitors for cancer therapy.
National University of Ireland Galway
Trends in targeting Bcl-2 anti-apoptotic proteins for cancer treatment.
Shenyang Pharmaceutical University
Scaffold hopping from indoles to indazoles yields dual MCL-1/BCL-2 inhibitors from MCL-1 selective leads.
University of Maryland
A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity.
Zhengzhou University
A novel Hsp70 inhibitor specifically targeting the cancer-related Hsp70-Bim protein-protein interaction.
Dalian University of Technology
Discovery of potent and selective Bcl-2 inhibitors with acyl sulfonamide skeleton.
Shanghai Institute of Pharmaceutical Industry
A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
Central South University
Targeting the Allosteric Pathway That Interconnects the Core-Functional Scaffold and the Distal Phosphorylation Sites for Specific Dephosphorylation of Bcl-2.
Dalian University of Technology
Sensitive fluorogenic substrates for sirtuin deacylase inhibitor discovery.
Xihua University
Synthesis and evaluation of a UMI-77-based fluorescent probe for selective detecting Mcl-1 protein and imaging in living cancer cells.
Shandong University
HDAC-Bax Multiple Ligands Enhance Bax-Dependent Apoptosis in HeLa Cells.
Shandong University
Pro-apoptotic carboxamide analogues of natural fislatifolic acid targeting Mcl-1 and Bcl-2.
Paris-Saclay University
Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.
Vanderbilt University School of Medicine
Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.
Servier Research Institute of Medicinal Chemistry
Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an α-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere.
TBA
Discovery and Characterization of 2,5-Substituted Benzoic Acid Dual Inhibitors of the Anti-apoptotic Mcl-1 and Bfl-1 Proteins.
National Institute of Chemistry
Clinical candidates modulating protein-protein interactions: The fragment-based experience.
Taros Chemicals
Design, synthesis and preliminary bioactivity studies of indomethacin derivatives as Bcl-2/Mcl-1 dual inhibitors.
Shandong University
Design, synthesis, and bioactivity evaluation of novel Bcl-2/HDAC dual-target inhibitors for the treatment of multiple myeloma.
Wuhan Polytechnic University
Proteolysis Targeting Chimeras for the Selective Degradation of Mcl-1/Bcl-2 Derived from Nonselective Target Binding Ligands.
TBA
Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics.
Dalian University of Technology
Design, synthesis and preliminary biological studies of pyrrolidine derivatives as Mcl-1 inhibitors.
Shandong University
Structure-based design of rhodanine-based acylsulfonamide derivatives as antagonists of the anti-apoptotic Bcl-2 protein.
Soochow University
Development of high potent and selective Bcl-2 inhibitors bearing the structural elements of natural product artemisinin.
Shanghai Institute of Materia Medica (Simm)
Discovery and development of substituted tyrosine derivatives as Bcl-2/Mcl-1 inhibitors.
Shandong University
Beyond the Rule of 5: Lessons Learned from AbbVie's Drugs and Compound Collection.
Abbvie
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.
Glaxosmithkline
Design, synthesis and pharmacological evaluation of new acyl sulfonamides as potent and selective Bcl-2 inhibitors.
Shanghai Institute of Materia Medica (Simm)
Dual inhibitors of the pro-survival proteins Bcl-2 and Mcl-1 derived from natural compound meiogynin A.
Paris-Saclay University
Expanding the Cancer Arsenal with Targeted Therapies: Disarmament of the Antiapoptotic Bcl-2 Proteins by Small Molecules.
University of Maryland
1-Phenyl-1H-indole derivatives as a new class of Bcl-2/Mcl-1 dual inhibitors: Design, synthesis, and preliminary biological evaluation.
Shandong University
Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia-1 Inhibitors Using Structure-Based Design.
Vanderbilt University School of Medicine
Discovery and structure-activity relationship studies of N-substituted indole derivatives as novel Mcl-1 inhibitors.
Shenyang Pharmaceutical University
FUSED PYRAZOLE UREA ANALOGS AS GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
Merck Sharp & Dohme
IMIDAZOCYCLIC COMPOUND AND APPLICATION THEREOF
Dongbao Purple Star (Hangzhou) Biopharmaceutical
THERAPY BASED ON SYNTHETIC LETHALITY IN SWI/SNF COMPLEX-DYSFUNCTION CANCER
National Cancer Center
Isoindoline compositions and methods for treating neurodegenerative disease
Cognition Therapeutics
Heteroaryl[4,3-C]pyrimidine-5-amine derivative, preparation method therefor, and medical uses thereof
Jiangsu Hengrui Medicine
Amino pyrazolopyrimidine compound used as neurotrophic factor tyrosine kinase receptor inhibitor
Chia Tai Tianqing Pharmaceutical Group
Compositions and methods for treating toxoplasmosis, cryptosporidiosis and other apicomplexan protozoan related diseases
University of Washington
Substituted pyrrolo[2,3-b]pyrazines and substituted pyrazolo[3,4-b]pyridines as ITK and JAK kinase inhibitors
Arrien Pharmaceuticals
Methods of modulating the activity of the MC5 receptor and treatment of conditions related to this receptor
Mimetica
Pharmacological characterization of human S1P4 using a novel radioligand, [4,5-3H]-dihydrosphingosine-1-phosphate.
Schering-Plough Research Institute
Pharmacological characterization of ZD6021: a novel, orally active antagonist of the tachykinin receptors.
Astrazeneca Pharmaceuticals
Rabbit alpha2-adrenoceptors: both platelets and adipocytes have alpha2A-pharmacology.
Glaxosmithkline
5HT4(a) and 5-HT4(b) receptors have nearly identical pharmacology and are both expressed in human atrium and ventricle.
University of Oslo
Novel bisubstrate analog inhibitors of serotonin N-acetyltransferase: the importance of being neutral.
Johns Hopkins University School of Medicine
Cloning of cDNAs encoding the human gamma-aminobutyric acid type A receptor alpha 6 subunit and characterization of the pharmacology of alpha 6-containing receptors.
Merck Sharp & Dohme Research Laboratories
Structural combination of established 5-HT(2A) receptor ligands: new aspects of the binding mode.
University of Mainz
7-[3-(4-[2,3-Dimethylphenyl]piperazinyl)propoxy]-2(1H)-quinolinone (OPC-4392), a presynaptic dopamine autoreceptor agonist and postsynaptic D2 receptor antagonist.
Tokushima Research Institute
Synthesis and target identification of hymenialdisine analogs.
Genomics Institute of The Novartis Research Foundation
4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.
Gsk