Journal of Medicinal Chemistry
Publication Venue For
Conformationally Defined Rexinoids for the Prevention of Inflammation and Nonmelanoma Skin Cancers
Structure-Activity Relationship Study of Momordica Saponin II Derivatives as Vaccine Adjuvants.
Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells.
Discovery of Potent, Selective, and In Vivo Efficacious AKT Kinase Protein Degraders via Structure-Activity Relationship Studies.
Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders.
Saturated Hydroxy Fatty Acids Exhibit a Cell Growth Inhibitory Activity and Suppress the Cytokine-Induced β-Cell Apoptosis
Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties
Molecule Property Analyses of Active Compounds for Mycobacterium tuberculosis
Structural Effect on Adjuvanticity of Saponins
Vaccine Adjuvants Derivatized from Momordica Saponins i and II
β-Lactones: A Novel Class of Ca
-Independent Phospholipase A
(Group VIA iPLA
) Inhibitors with the Ability To Inhibit β-Cell Apoptosis
Synthesis and Evaluation of a QS-17/18-Based Vaccine Adjuvant
Molecular Mechanism of Inhibition of Acid Ceramidase by Carmofur.
Proline- and arginine-rich peptides as flexible allosteric modulators of human proteasome activity
A-C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions.
Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH)
Synthesis and Antiviral Evaluation of Octadecyloxyethyl Benzyl 9-[(2-Phosphonomethoxy)ethyl]guanine (ODE-Bn-PMEG), a Potent Inhibitor of Transient HPV DNA Amplification
Synthesis and Biological Evaluation of Vitamin D3 Metabolite 20S,23S-Dihydroxyvitamin D3 and Its 23R Epimer
Effect of α-Methyl versus α-Hydrogen Substitution on Brain Availability and Tumor Imaging Properties of Heptanoic [F-18]Fluoroalkyl Amino Acids for Positron Emission Tomography (PET)
Chemical Synthesis and Biological Activities of 20S,24S/R-Dihydroxyvitamin D3 Epimers and Their 1α-Hydroxyl Derivatives
Conformationally Defined Rexinoids and Their Efficacy in the Prevention of Mammary Cancers
Synthesis and Biological Evaluation of (S)-Amino-2-methyl-4-[
Br]bromo-3-(E)-butenoic Acid (BrVAIB) for Brain Tumor Imaging
Synthesis, Radiolabeling, and Biological Evaluation of (R)- and (S)-2-Amino-5-[(18)F]fluoro-2-methylpentanoic Acid ((R)-, (S)-[(18)F]FAMPe) as Potential Positron Emission Tomography Tracers for Brain Tumors.
Discovery of potent inhibitors of Schistosoma mansoni NAD
Exploration of cyanine compounds as selective inhibitors of protein arginine methyltransferases: Synthesis and biological evaluation
Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1
Design and in vitro activities of N -alkyl- N -[(8- R -2,2-dimethyl-2 H -chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents
Design, synthesis, and biological action of 20 R -hydroxyvitamin D3
Novel targeted system to deliver chemotherapeutic drugs to EphA2-expressing cancer cells
Design and synthesis of novel small-molecule inhibitors of the hypoxia inducible factor pathway
Identification of inhibitors that block vaccinia virus infection by targeting the DNA synthesis processivity factor D4
Acyloxy nitroso compounds as nitroxyl (HNO) donors: Kinetics, reactions with thiols, and vasodilation properties
A synthetic 7,8-dihydroxyflavone derivative promotes neurogenesis and exhibits potent antidepressant effect.
Synthesis and biological evaluation of apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins
BI-97C1, an optically pure apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/Leukemia-2 (Bcl-2) family proteins
Synthesis and preliminary biological evaluation of high-drug-load paclitaxel-antibody conjugates for tumor-targeted chemotherapy
Synthesis, radiolabeling, and biological evaluation of (R)- and (S)-2-amino-3-[(18)F]fluoro-2-methylpropanoic acid (FAMP) and (R)- and (S)-3-[(18)F]fluoro-2-methyl-2-N-(methylamino)propanoic acid (NMeFAMP) as potential PET radioligands for imaging brain tumors.
New insights into the design of inhibitors of human S-adenosylmethionine decarboxylase: studies of adenine C
substitution in structural analogues of S-adenosylmethionine
Structure-activity relationships of 7-deaza-6-benzylthioinosine analogues as ligands of Toxoplasma gondii adenosine kinase
Design and development of water-soluble curcumin conjugates as potential anticancer agents
Design, synthesis, and characterization of a dual modality positron emission tomography and fluorescence imaging agent for monoclonal antibody tumor-targeted imaging
Novel boron-containing, nonclassical antifolates: Synthesis and preliminary biological and structural evaluation
Antibacterial nicotinamide adenine dinucleotide synthetase inhibitors: Amide- and ether-linked tethered dimers with α-amino acid end groups
Using fragment cocktail crystallography to assist inhibitor design of Trypanosoma brucei nucleoside 2-deoxyribosyltransferase
Evaluation of carbon-11-labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-iodoethenyl)phenyl]nortropane as a potential radioligand for imaging the serotonin transporter by PET.
Inhibition of carboxylesterases by benzil (diphenylethane-1,2-dione) and heterocyclic analogues is dependent upon the aromaticity of the ring and the flexibility of the dione moiety
Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands.
Identification and characterization of novel benzil (diphenylethane-1,2- dione) analogues as inhibitors of mammalian carboxylesterases
Identification of 1,2,3,4,5,6-hexabromocyclohexane as a small molecule inhibitor of Jak2 tyrosine kinase autophophorylation
Synthesis and structure-activity relationship studies for hydantoins and analogues as voltage-gated sodium channel ligands
Syntheses and Neuraminidase Inhibitory Activity of Multisubstituted Cyclopentane Amide Derivatives
Synthesis, Biological Activity and Molecular Modeling of 6-Benzylthioinosine Analogues as Subversive Substrates of Toxoplasma gondii Adenosine Kinase
Synthesis, radiosynthesis, and biological evaluation of carbon-11 and iodine-123 labeled 2beta-carbomethoxy-3beta-[4'-((Z)-2-haloethenyl)phenyl]tropanes: candidate radioligands for in vivo imaging of the serotonin transporter.
Antimycobacterial Agents. 1. Thio Analogues of Purine
Conformationally defined retinoic acid analogues. 5. Large-scale synthesis and mammary cancer chemopreventive activity for (2E,4E,6Z,8E)-8-(3′,4′-dihydro-1′(2′H) -naphthalen-1′-ylidene)-3,7-dimethyl-2,4,6-octatrienoic acid (9cUAB30)
Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone
Tethered dimers as NAD synthetase inhibitors with antibacterial activity
Synthesis and characterization of iodine-123 labeled 2beta-carbomethoxy-3beta-(4'-((Z)-2-iodoethenyl)phenyl)nortropane. A ligand for in vivo imaging of serotonin transporters by single-photon-emission tomography.
Synthesis and antimycobacterial activity of pyrazine and quinoxaline derivatives
Enhancement of nucleoside cytotoxicity through nucleotide prodrugs
Radiolabeled amino acids for tumor imaging with PET: radiosynthesis and biological evaluation of 2-amino-3-[18F]fluoro-2-methylpropanoic acid and 3-[18F]fluoro-2-methyl-2-(methylamino)propanoic acid.
Synthesis of syn- and anti-1-amino-3-[18F]fluoromethyl-cyclobutane-1-carboxylic acid (FMACBC), potential PET ligands for tumor detection.
Synthesis and evaluation of several new (2-chloroethyl)nitrosocarbamates as potential anticancer agents
Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2β-carbo-1'-fluoro-2-propoxy-3β-(4-chlorophenyl)tropanes. Ligands for the imaging of dopamine transporters by positron emission tomography
Paclitaxel derivatives for targeted therapy of cancer: Toward the development of smart taxanes
Potent inhibition of influenza sialidase by a benzoic acid containing a 2-pyrrolidinone substituent
Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel
Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y
receptor antagonists and partial agonists
Synthesis and biological activity of certain 4'-thio-D- arabinofuranosylpurine nucleosides
Conformationally defined retinoic acid analogues. 4. Potential new agents for acute promyelocytic and juvenile myelomonocytic leukemias
Effects of log P and phenyl ring conformation on the binding of 5- phenylhydantoins to the voltage-dependent sodium channel
Conformationally defined 6-s-trans-retinoic acid analogs. 3. Structure- activity relationships for nuclear receptor binding, transcriptional activity, and cancer chemopreventive activity
Structure-Based Inhibitors of Inñuenza Virus Sialidase. A Benzoic Acid Lead with Novel Interaction
Conformationally Defined 6-s-trans-Retinoic Acid Analogs. 2. Selective Agonists for Nuclear Receptor Binding and Transcriptional Activity
Search for New Purine- and Ribose-Modified Adenosine Analogues as Selective Agonists and Antagonists at Adenosine Receptors
A Conformationally Defined 6-s-trans-Retinoic Acid Isomer: Synthesis, Chemopreventive Activity, and Toxicity
3-Amino-5,5-dimethylhexanoic Acid. Synthesis, Resolution, and Effects on Carnitine Acyltransferases
Bicyclic Hydantoins with a Bridgehead Nitrogen. Comparison of Anticonvulsant Activities with Binding to the Neuronal Voltage-Dependent Sodium Channel
Additions and Corrections: Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 3. 9-Arylmethyl Derivatives of 9-Deazaguanine Substituted on the Methylene Group ((J. Med. Chem. (1993) 36(24) (3771–3783) (10.1021/jm00076a004))
Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 4. A Study of Phosphate Mimics
Phosphonate Analogs of Carbocyclic Nucleotides
Phenylselenenyl- and Phenylthio-Substituted Pyrimidines as Inhibitors of Dihydrouracil Dehydrogenase and Uridine Phosphorylase
Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 1. 9-(Arylmethyl) Derivatives of 9-Deazaguanine
Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 2. 9-Alicyclic and 9-Heteroalicyclic Derivatives of 9-Deazaguanine
Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 3. 9-Arylmethyl Derivatives of 9-Deazaguanine Substituted on the Methylene Group
Syntheses of 5′-Substituted Analogues of Carbocyclic 3-Deazaadenosine as Potential Antivirals
5,5-Disubstituted Hydantoins: Syntheses and Anti-HIV Activity
Synthesis and Antiviral Evaluation of N-Carboxamidine-Substituted Analogs of 1-β-D-Ribofuranosyl-1,2,4-triazole-3-carboxamidine Hydrochloride
Small Atrial Natriuretic Peptide Analogs: Design, Synthesis, and Structural Requirements for Guanylate Cyclase Activation
Synthesis and Anti-HIV Activity of 4′-Thio-2′,3′-dideoxynucleosides
Synthesis and Biological Activity of 2′-Fluoro-2-halo Derivatives of 9-β-d-Arabinofuranosyladenine
Synthesis and Biological Activity of 2′-Deoxy-4′-thio Pyrimidine Nucleosides
Effect of structural modifications in the C7-C11 region of the retinoid skeleton on biological activity in a series of aromatic retinoids.
Sodium Channel Binding and Anticonvulsant Activities for the Enantiomers of t Bicyclic 2,4-Oxazolidinedione and Monocyclic Models
Anticonvulsant Activities of Phenyl-Substituted Bicyclic 2,4-Oxazolidinediones and Monocyclic Models. Comparison with Binding to the Neuronal Voltage-Dependent Sodium Channel
Synthesis and Biological Evaluations of Certain 2-Halo-2'-Substituted Derivatives of 9-β-D-Arabinofuranosyladenine
Resolution of Racemic Carbocyclic Analogues of Purine Nucleosides through the Action of Adenosine Deaminase. Antiviral Activity of the Carbocyclic 2′-Deoxyguanosine Enantiomers
9-(2-Deoxy-2-fluoro-3-D-arabinofuranosy1)guanine: A Metabolically Stable Cytotoxic Analogue of 2’-Deoxyguanosine
Synthesis and Biochemical Properties of 8-Amino-6-fluoro-9-β-D-ribofuranosyl-9H-purine
2-Fluoroformycin and 2-Aminoformycin. Synthesis and Biological Activity
(±)-3-(4-Amino-lif-pyrrolo[2,3-d]pyrimidin-l-yl)-5-(hydroxymethyl)-(lα,2α,3β,5β)-1,2-cyclopentanediol, the Carbocyclic Analogue of Tubercidin
Identification of an Acridine Photoaffinity Probe for Trypanocidal Action
Improved Synthesis And Antitumor Activity Of 2-Bromo-2'-Deoxyadenosine
Synthesis and Anticonvulsant Activity of Some Substituted Lactams and Amides
Synthesis and Biological Evaluation of 2-Fluoro-8-azaadenosine and Related Compounds
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