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JOURNAL OF MEDICINAL CHEMISTRY
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Overview
publication venue for
Brain-Permeable Immunoproteasome-Targeting Macrocyclic Peptide Epoxyketones for Alzheimer's Disease
. 67:7146-7157.
2024
Discovery of Anthranilic Acid Derivatives as Difluoromethylornithine Adjunct Agents That Inhibit Far Upstream Element Binding Protein 1 (FUBP1) Function
. 65:15391-15415.
2022
Development of a Redox-Sensitive Spermine Prodrug for the Potential Treatment of Snyder Robinson Syndrome
. 64:15593-15607.
2021
Functional Mixture-Based Positional Scan Identifies a Library of Antagonist Tetrapeptide Sequences (LAtTeS) with Nanomolar Potency for the Melanocortin-4 Receptor and Equipotent with the Endogenous AGRP(86-132) Antagonist
. 64:14860-14875.
2021
Macrocyclic Immunoproteasome Inhibitors as a Potential Therapy for Alzheimer's Disease
. 64:10934-10950.
2021
Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High-Throughput "Unbiased" Screening Campaign
. 64:5577-5592.
2021
LMP2 Inhibitors as a Potential Treatment for Alzheimer's Disease
. 63:3763-3783.
2020
Preclinical Optimization of gp120 Entry Antagonists as anti-HIV-1 Agents with Improved Cytotoxicity and ADME Properties through Rational Design, Synthesis, and Antiviral Evaluation
. 63:1724-1749.
2020
Development of Novel Epoxyketone-Based Proteasome Inhibitors as a Strategy To Overcome Cancer Resistance to Carfilzomib and Bortezomib
. 62:4444-4455.
2019
Discovery of Polypharmacological Melanocortin-3 and -4 Receptor Probes and Identification of a 100-Fold Selective nM MC3R Agonist versus a μm MC4R Partial Agonist
. 62:2738-2749.
2019
Pyridinium Oximes with
Ortho
-Positioned Chlorine Moiety Exhibit Improved Physicochemical Properties and Efficient Reactivation of Human Acetylcholinesterase Inhibited by Several Nerve Agents
. 61:10753-10766.
2018
Highly Selective and Potent α4β2 nAChR Antagonist Inhibits Nicotine Self-Administration and Reinstatement in Rats
. 60:10092-10104.
2017
Selective Inhibition of
Escherichia coli
RNA and DNA Topoisomerase I by Hoechst 33258 Derived Mono- and Bisbenzimidazoles
. 60:4904-4922.
2017
Discovery of Mixed Pharmacology Melanocortin-3 Agonists and Melanocortin-4 Receptor Tetrapeptide Antagonist Compounds (TACOs) Based on the Sequence Ac-Xaa
1
-Arg-(pI)DPhe-Xaa
4
-NH
2
. 60:4342-4357.
2017
Synthesis, Antiviral Potency, in Vitro ADMET, and X-ray Structure of Potent CD4 Mimics as Entry Inhibitors That Target the Phe43 Cavity of HIV-1 gp120
. 60:3124-3153.
2017
Potent μ-Opioid Receptor Agonists from Cyclic Peptides Tyr-c[ d -Lys-Xxx-Tyr-Gly]: Synthesis, Biological, and Structural Evaluation
. 59:1239-1245.
2016
Structure-Based Design of a Small Molecule CD4-Antagonist with Broad Spectrum Anti-HIV-1 Activity
. 58:6909-6927.
2015
SAR Studies of Exosite-Binding Substrate-Selective Inhibitors of A Disintegrin And Metalloprotease 17 (ADAM17) and Application as Selective in Vitro Probes
. 58:5808-5824.
2015
Parallel Synthesis of Hexahydrodiimidazodiazepines Heterocyclic Peptidomimetics and Their in Vitro and in Vivo Activities at μ (MOR), δ (DOR), and κ (KOR) Opioid Receptors
. 58:4905-4917.
2015
Combinatorial Libraries As a Tool for the Discovery of Novel, Broad-Spectrum Antibacterial Agents Targeting the ESKAPE Pathogens
. 58:3340-3355.
2015
Proteasome inhibitors with pyrazole scaffolds from structure-based virtual screening
. 58:2036-2041.
2015
Synthesis, Structure-Activity Relationship Studies, and Antibacterial Evaluation of 4-Chromanones and Chalcones, as Well as Olympicin A and Derivatives
. 57:8398-8420.
2014
Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes
. 57:6197-6209.
2014
Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R Human Melanocortin-4 Polymorphic Receptors (hMC4Rs)
. 57:4615-4628.
2014
Discovery of a potent and selective α3β4 nicotinic acetylcholine receptor antagonist from an α-conotoxin synthetic combinatorial library
. 57:3511-3521.
2014
Novel pyrrolidine diketopiperazines selectively inhibit melanoma cells via induction of late-onset apoptosis
. 57:1599-1608.
2014
Synthesis and Cytostatic Evaluation of 4-
N
-Alkanoyl and 4-
N
-Alkyl Gemcitabine Analogues
. 57:191-203.
2014
Scaffold Ranking and Positional Scanning Utilized in the Discovery of nAChR-Selective Compounds Suitable for Optimization Studies
. 56:10103-10117.
2013
The multi-leu peptide inhibitor discriminates between PACE4 and furin and exhibits antiproliferative effects on prostate cancer cells
. 55:10501-10511.
2012
Synthesis, Biological Evaluation, X-ray Structure, and Pharmacokinetics of Aminopyrimidine c-jun-N-terminal Kinase (JNK) Inhibitors
. 53:419-431.
2010
Directed discovery of agents targeting the met tyrosine kinase domain by virtual screening
. 52:943-951.
2009
Antagonists of the Human A
2A
Adenosine Receptor. 4. Design, Synthesis, and Preclinical Evaluation of 7-Aryltriazolo[4,5-
d
]pyrimidines
. 52:33-47.
2009
Selectivity and mechanism of action of a growth factor receptor-bound protein 2 Src homology 2 domain binding antagonist
. 51:7459-7468.
2008
Design and microwave-assisted synthesis of novel macrocyclic peptides active at melanocortin receptors: Discovery of potent and selective hMC5R receptor antagonists
. 51:2701-2707.
2008
Design of a potent reactivator of tabun-inhibited acetyleholinesterase-synthesis and evaluation of (
E
)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203)
. 50:5514-5518.
2007
Antitrypanosomal activity of 5 '-deoxy-5 '-(iodomethylene)adenosine and related 6-N-cyclopropyladenosine analogues
. 49:2096-2102.
2006
Development of cyclic gamma-MSH analogues with selective hMC3R agonist and hMC3R/hMC5R antagonist activities
. 49:1946-1952.
2006
Are L-adenosine and its derivatives substrates for S-adenosyl-L-homocysteine hydrolase?
. 48:3649-3653.
2005
Stereoselective synthesis of sugar-modified enyne analogues of adenosine and uridine.: Interaction with
S
-adenosyl-L-homocysteine hydrolase and antiviral and cytotoxic effects
. 47:5251-5257.
2004
Synthesis and aromatase inhibitory activity of novel pyridine-containing isoflavones
. 47:4032-4040.
2004
Sugar-modified conjugated diene analogues of adenosine and uridine:: Synthesis, interaction with
S
-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects
. 45:2651-2658.
2002
Doubly homologated dihalovinyl and acetylene analogues of adenosine:: Synthesis, interaction with
S
-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects
. 43:1180-1186.
2000
Inactivation of
S
-adenosyl-L-homocysteine hydrolase and antiviral activity with 5′,5′,6′,6′-tetradehydro-6′-deoxy-6′-halohomoadenosine analogues (4′-haloacetylene analogues derived from adenosine)
. 41:3857-3864.
1998
Discovery of type II (covalent) inactivation of S-adenosyl-L-homocysteine hydrolase involving its "hydrolytic activity": Synthesis and evaluation of dihalohomovinyl nucleoside analogues derived from adenosine
. 41:3078-3083.
1998
Anticancer and antiviral effects and inactivation of S-adenosyl-L-homocysteine hydrolase with 5'-carboxaldehydes and oximes synthesized from adenosine and sugar-modified analogues
. 40:1608-1618.
1997
Structure-based design of a new bisintercalating anthracycline antibiotic
. 40:261-266.
1997
Inactivation of S-adenosyl-L-homocysteine hydrolase by amide and ester derivatives of adenosine-5'-carboxylic acid
. 39:4162-4166.
1996
NUCLEIC-ACID RELATED-COMPOUNDS .84. SYNTHESIS OF 6'-(E AND Z)-HALOHOMOVINYL DERIVATIVES OF ADENOSINE, INACTIVATION OF S-ADENOSYL-L-HOMOCYSTEINE HYDROLASE, AND CORRELATION OF ANTICANCER AND ANTIVIRAL POTENCIES WITH ENZYME-INHIBITION
. 37:3579-3587.
1994
POLYACRYLAMIDES BEARING PENDANT ALPHA-SIALOSIDE GROUPS STRONGLY INHIBIT AGGLUTINATION OF ERYTHROCYTES BY INFLUENZA-A VIRUS - MULTIVALENCY AND STERIC STABILIZATION OF PARTICULATE BIOLOGICAL-SYSTEMS
. 37:3419-3433.
1994
ADENOSINE-5'-CARBOXALDEHYDE - A POTENT INHIBITOR OF S-ADENOSYL-L-HOMOCYSTEINE HYDROLASE
. 36:883-887.
1993
Synthesis of Pure p-Chlorophenyl-L-alanine form L-Phenylalanine
. 17:556-558.
1974
APPLICATION OF SEQUENTIAL SIMPLEX METHOD IN DESIGNING DRUG ANALOGS
. 17:799-804.
1974
Chemical genetics: Exploring the role of the proteasome in cell biology using natural products and other small molecule proteasome inhibitors
2008
Correction to "Macrocyclic Immunoproteasome Inhibitors as a Potential Therapy for Alzheimer's Disease".
2024
Erratum: Discovery of Nanomolar Melanocortin-3 Receptor (MC3R)-Selective Small Molecule Pyrrolidine Bis-Cyclic Guanidine Agonist Compounds Via a High Throughput 'Unbiased' Screening Campaign (J. Med. Chem. (2021) 64:9 (5577−5592) DOI: 10.1021/acs.jmedchem.0c02041)
2023
Identification of the 4-Position of 3-Alkynyl and 3-Heteroaromatic Substituted Pyridine Methanamines as a Key Modification Site Eliciting Increased Potency and Enhanced Selectivity for Cytochrome P-450 2A6 Inhibition.
2018
Correction to Synthesis, Antiviral Potency, in Vitro ADMET, and X-ray Structure of Potent CD4 Mimics as Entry Inhibitors That Target the Phe43 Cavity of HIV-1 gp120.
2017
Synthesis, Biological Evaluation, X-ray Structure, and Pharmacokinetics of Aminopyrimidine c-jun-N-terminal Kinase (JNK) Inhibitors (vol 53, pg 419, 2010)
2010
Mixture-based synthetic combinatorial libraries
1999
Research
category
CHEMISTRY, MEDICINAL
Category
Identifiers
International Standard Serial Number (ISSN)
0022-2623
Electronic International Standard Serial Number (EISSN)
1520-4804
Other
journal abbreviation
J MED CHEM
