Journal of Medicinal Chemistry

Conformationally Defined Rexinoids for the Prevention of Inflammation and Nonmelanoma Skin Cancers.  65:14409-14423. 2022

Structure-Activity Relationship Study of Momordica Saponin II Derivatives as Vaccine Adjuvants.  65:14589-14598. 2022

Novel Allosteric Inhibitor-Derived AKT Proteolysis Targeting Chimeras (PROTACs) Enable Potent and Selective AKT Degradation in KRAS/BRAF Mutant Cells..  65:14237-14260. 2022

Discovery of Potent, Selective, and In Vivo Efficacious AKT Kinase Protein Degraders via Structure-Activity Relationship Studies..  65:3644-3666. 2022

Design, Synthesis, and Evaluation of Potent, Selective, and Bioavailable AKT Kinase Degraders..  64:18054-18081. 2021

Saturated Hydroxy Fatty Acids Exhibit a Cell Growth Inhibitory Activity and Suppress the Cytokine-Induced β-Cell Apoptosis.  63:12666-12681. 2020

Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties.  63:10984-11011. 2020

Molecule Property Analyses of Active Compounds for Mycobacterium tuberculosis.  63:8917-8955. 2020

Structural Effect on Adjuvanticity of Saponins.  63:3290-3297. 2020

Vaccine Adjuvants Derivatized from Momordica Saponins i and II.  62:9976-9982. 2019

β-Lactones: A Novel Class of Ca ²⁺ -Independent Phospholipase A 2 (Group VIA iPLA 2 ) Inhibitors with the Ability To Inhibit β-Cell Apoptosis.  62:2916-2927. 2019

Synthesis and Evaluation of a QS-17/18-Based Vaccine Adjuvant.  62:1669-1676. 2019

Molecular Mechanism of Inhibition of Acid Ceramidase by Carmofur..  62:987-992. 2019

Proline- and arginine-rich peptides as flexible allosteric modulators of human proteasome activity 2018

A-C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions.  61:4720-4738. 2018

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).  60:9184-9204. 2017

Retraction of "Design and Synthesis of Novel Cyclic Amine Benzimidazoles for the Treatment of Pancreatic Cancer"..  60:7615. 2017

Synthesis and Antiviral Evaluation of Octadecyloxyethyl Benzyl 9-[(2-Phosphonomethoxy)ethyl]guanine (ODE-Bn-PMEG), a Potent Inhibitor of Transient HPV DNA Amplification.  59:10470-10478. 2016

Synthesis and Biological Evaluation of Vitamin D3 Metabolite 20S,23S-Dihydroxyvitamin D3 and Its 23R Epimer.  59:5102-5108. 2016

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).  59:3515-3531. 2016

Chemical Synthesis and Biological Activities of 20S,24S/R-Dihydroxyvitamin D3 Epimers and Their 1α-Hydroxyl Derivatives.  58:7881-7887. 2015

Conformationally Defined Rexinoids and Their Efficacy in the Prevention of Mammary Cancers.  58:7763-7774. 2015

Synthesis and Biological Evaluation of (S)-Amino-2-methyl-4-[⁷⁶Br]bromo-3-(E)-butenoic Acid (BrVAIB) for Brain Tumor Imaging.  58:8542-8552. 2015

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..  58:3817-3829. 2015

Discovery of potent inhibitors of Schistosoma mansoni NAD⁺ catabolizing enzyme.  58:3582-3592. 2015

Exploration of cyanine compounds as selective inhibitors of protein arginine methyltransferases: Synthesis and biological evaluation.  58:1228-1243. 2015

Methyl substitution of a rexinoid agonist improves potency and reveals site of lipid toxicity.  57:5370-5380. 2014

Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.  57:2611-2622. 2014

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.  55:6738-6750. 2012

Design, synthesis, and biological action of 20 R -hydroxyvitamin D3.  55:3573-3577. 2012

Novel targeted system to deliver chemotherapeutic drugs to EphA2-expressing cancer cells.  55:2427-2436. 2012

Design and synthesis of novel small-molecule inhibitors of the hypoxia inducible factor pathway.  54:8471-8489. 2011

Identification of inhibitors that block vaccinia virus infection by targeting the DNA synthesis processivity factor D4.  54:3260-3267. 2011

Acyloxy nitroso compounds as nitroxyl (HNO) donors: Kinetics, reactions with thiols, and vasodilation properties.  54:1059-1070. 2011

A synthetic 7,8-dihydroxyflavone derivative promotes neurogenesis and exhibits potent antidepressant effect..  53:8274-8286. 2010

Synthesis and biological evaluation of apogossypolone derivatives as pan-active inhibitors of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins.  53:8000-8011. 2010

BI-97C1, an optically pure apogossypol derivative as pan-active inhibitor of antiapoptotic B-cell lymphoma/Leukemia-2 (Bcl-2) family proteins.  53:4166-4176. 2010

Synthesis and preliminary biological evaluation of high-drug-load paclitaxel-antibody conjugates for tumor-targeted chemotherapy.  53:586-594. 2010

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..  53:876-886. 2010

New insights into the design of inhibitors of human S-adenosylmethionine decarboxylase: studies of adenine C ⁸ substitution in structural analogues of S-adenosylmethionine.  52:1388-1407. 2009

Structure-activity relationships of 7-deaza-6-benzylthioinosine analogues as ligands of Toxoplasma gondii adenosine kinase.  51:3934-3945. 2008

Design and development of water-soluble curcumin conjugates as potential anticancer agents.  50:6284-6288. 2007

Design, synthesis, and characterization of a dual modality positron emission tomography and fluorescence imaging agent for monoclonal antibody tumor-targeted imaging.  50:4759-4765. 2007

Novel boron-containing, nonclassical antifolates: Synthesis and preliminary biological and structural evaluation.  50:3283-3289. 2007

Antibacterial nicotinamide adenine dinucleotide synthetase inhibitors: Amide- and ether-linked tethered dimers with α-amino acid end groups.  50:2612-2621. 2007

Using fragment cocktail crystallography to assist inhibitor design of Trypanosoma brucei nucleoside 2-deoxyribosyltransferase.  49:5939-5946. 2006

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..  49:942-946. 2006

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.  48:5543-5550. 2005

Synthesis, in vitro characterization, and radiolabeling of N,N-dimethyl-2-(2'-amino-4'-substituted-phenylthio)benzylamines: potential candidates as selective serotonin transporter radioligands..  48:4254-4265. 2005

Identification and characterization of novel benzil (diphenylethane-1,2- dione) analogues as inhibitors of mammalian carboxylesterases.  48:2906-2915. 2005

Identification of 1,2,3,4,5,6-hexabromocyclohexane as a small molecule inhibitor of Jak2 tyrosine kinase autophophorylation.  48:2526-2533. 2005

Synthesis and structure-activity relationship studies for hydantoins and analogues as voltage-gated sodium channel ligands.  47:6519-6528. 2004

Syntheses and Neuraminidase Inhibitory Activity of Multisubstituted Cyclopentane Amide Derivatives.  47:1919-1929. 2004

Synthesis, Biological Activity and Molecular Modeling of 6-Benzylthioinosine Analogues as Subversive Substrates of Toxoplasma gondii Adenosine Kinase.  47:1987-1996. 2004

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..  47:1122-1135. 2004

Antimycobacterial Agents. 1. Thio Analogues of Purine.  47:273-276. 2004

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).  46:3766-3769. 2003

Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.  46:3865-3876. 2003

Tethered dimers as NAD synthetase inhibitors with antibacterial activity.  46:3371-3381. 2003

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..  46:925-935. 2003

Synthesis and antimycobacterial activity of pyrazine and quinoxaline derivatives.  45:5604-5606. 2002

Enhancement of nucleoside cytotoxicity through nucleotide prodrugs.  45:4505-4512. 2002

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..  45:2240-2249. 2002

Synthesis of syn- and anti-1-amino-3-[18F]fluoromethyl-cyclobutane-1-carboxylic acid (FMACBC), potential PET ligands for tumor detection..  45:2250-2259. 2002

Synthesis and evaluation of several new (2-chloroethyl)nitrosocarbamates as potential anticancer agents.  43:1484-1488. 2000

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.  43:639-648. 2000

Paclitaxel derivatives for targeted therapy of cancer: Toward the development of smart taxanes.  42:4919-4924. 1999

Potent inhibition of influenza sialidase by a benzoic acid containing a 2-pyrrolidinone substituent.  42:2332-2343. 1999

Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel.  42:1537-1545. 1999

Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonists.  42:1625-1638. 1999

Synthesis and biological activity of certain 4'-thio-D- arabinofuranosylpurine nucleosides.  41:3865-3871. 1998

Conformationally defined retinoic acid analogues. 4. Potential new agents for acute promyelocytic and juvenile myelomonocytic leukemias.  41:1679-1687. 1998

Effects of log P and phenyl ring conformation on the binding of 5- phenylhydantoins to the voltage-dependent sodium channel.  40:602-607. 1997

Conformationally defined 6-s-trans-retinoic acid analogs. 3. Structure- activity relationships for nuclear receptor binding, transcriptional activity, and cancer chemopreventive activity.  39:3625-3635. 1996

Structure-Based Inhibitors of Inñuenza Virus Sialidase. A Benzoic Acid Lead with Novel Interaction.  38:3217-3225. 1995

Conformationally Defined 6-s-trans-Retinoic Acid Analogs. 2. Selective Agonists for Nuclear Receptor Binding and Transcriptional Activity.  38:2302-2310. 1995

Search for New Purine- and Ribose-Modified Adenosine Analogues as Selective Agonists and Antagonists at Adenosine Receptors.  38:1174-1188. 1995

A Conformationally Defined 6-s-trans-Retinoic Acid Isomer: Synthesis, Chemopreventive Activity, and Toxicity.  37:4499-4507. 1994

3-Amino-5,5-dimethylhexanoic Acid. Synthesis, Resolution, and Effects on Carnitine Acyltransferases.  37:3247-3251. 1994

Bicyclic Hydantoins with a Bridgehead Nitrogen. Comparison of Anticonvulsant Activities with Binding to the Neuronal Voltage-Dependent Sodium Channel.  37:3289-3293. 1994

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)).  37:1034. 1994

Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 4. A Study of Phosphate Mimics.  37:1109-1114. 1994

Phosphonate Analogs of Carbocyclic Nucleotides.  37:739-744. 1994

Phenylselenenyl- and Phenylthio-Substituted Pyrimidines as Inhibitors of Dihydrouracil Dehydrogenase and Uridine Phosphorylase.  36:4250-4254. 1993

Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 1. 9-(Arylmethyl) Derivatives of 9-Deazaguanine.  36:55-69. 1993

Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 2. 9-Alicyclic and 9-Heteroalicyclic Derivatives of 9-Deazaguanine.  36:1847-1854. 1993

Structure-Based Design of Inhibitors of Purine Nucleoside Phosphorylase. 3. 9-Arylmethyl Derivatives of 9-Deazaguanine Substituted on the Methylene Group.  36:3771-3783. 1993

Syntheses of 5′-Substituted Analogues of Carbocyclic 3-Deazaadenosine as Potential Antivirals.  36:2102-2106. 1993

5,5-Disubstituted Hydantoins: Syntheses and Anti-HIV Activity.  35:3567-3572. 1992

Synthesis and Antiviral Evaluation of N-Carboxamidine-Substituted Analogs of 1-β-D-Ribofuranosyl-1,2,4-triazole-3-carboxamidine Hydrochloride.  35:3231-3238. 1992

Small Atrial Natriuretic Peptide Analogs: Design, Synthesis, and Structural Requirements for Guanylate Cyclase Activation.  35:808-816. 1992

Synthesis and Anti-HIV Activity of 4′-Thio-2′,3′-dideoxynucleosides.  35:533-538. 1992

Synthesis and Biological Activity of 2′-Fluoro-2-halo Derivatives of 9-β-d-Arabinofuranosyladenine.  35:397-401. 1992

Synthesis and Biological Activity of 2′-Deoxy-4′-thio Pyrimidine Nucleosides.  34:2361-2366. 1991

Effect of structural modifications in the C7-C11 region of the retinoid skeleton on biological activity in a series of aromatic retinoids..  32:1504-1517. 1989

Sodium Channel Binding and Anticonvulsant Activities for the Enantiomers of t Bicyclic 2,4-Oxazolidinedione and Monocyclic Models.  32:1577-1580. 1989

Anticonvulsant Activities of Phenyl-Substituted Bicyclic 2,4-Oxazolidinediones and Monocyclic Models. Comparison with Binding to the Neuronal Voltage-Dependent Sodium Channel.  31:2218-2221. 1988

Synthesis and Biological Evaluations of Certain 2-Halo-2'-Substituted Derivatives of 9-β-D-Arabinofuranosyladenine.  31:405-410. 1988

Resolution of Racemic Carbocyclic Analogues of Purine Nucleosides through the Action of Adenosine Deaminase. Antiviral Activity of the Carbocyclic 2′-Deoxyguanosine Enantiomers.  30:746-749. 1987

9-(2-Deoxy-2-fluoro-3-D-arabinofuranosy1)guanine: A Metabolically Stable Cytotoxic Analogue of 2’-Deoxyguanosine.  29:2389-2392. 1986

Synthesis and Biochemical Properties of 8-Amino-6-fluoro-9-β-D-ribofuranosyl-9H-purine.  29:2069-2074. 1986

2-Fluoroformycin and 2-Aminoformycin. Synthesis and Biological Activity.  28:1740-1742. 1985

(±)-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.  27:534-536. 1984

Identification of an Acridine Photoaffinity Probe for Trypanocidal Action.  27:865-870. 1984

Improved Synthesis And Antitumor Activity Of 2-Bromo-2'-Deoxyadenosine.  27:800-802. 1984

Synthesis and Anticonvulsant Activity of Some Substituted Lactams and Amides.  27:202-206. 1984

Synthesis and Biological Evaluation of 2-Fluoro-8-azaadenosine and Related Compounds.  26:1483-1489. 1983