Journal of Medicinal Chemistry Journal

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Discovery of First-in-Class PROTAC Degraders of SARS-CoV-2 Main Protease. 2024
Piptide Chemotypes for Perturbation of the Interaction of Urokinase with Its Receptor.. 65:12925-12932. 2022
Evolutionary and Structural Insights about Potential SARS-CoV-2 Evasion of Nirmatrelvir.. 65:8686-8698. 2022
Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target.. 65:409-423. 2022
Self-Masked Aldehyde Inhibitors: A Novel Strategy for Inhibiting Cysteine Proteases.. 64:11267-11287. 2021
Discovery of Selective Small-Molecule Inhibitors for the ENL YEATS Domain.. 64:10997-11013. 2021
HER2 Kinase-Targeted Breast Cancer Therapy: Design, Synthesis, and In Vitro and In Vivo Evaluation of Novel Lapatinib Congeners as Selective and Potent HER2 Inhibitors with Favorable Metabolic Stability.. 63:15906-15945. 2020
Nature-Inspired (di)Azine-Bridged Bisindole Alkaloids with Potent Antibacterial In Vitro and In Vivo Efficacy against Methicillin-Resistant Staphylococcus aureus.. 63:12623-12641. 2020
Confronting Racism in Chemistry Journals.. 63:6575-6577. 2020
Update to Our Reader, Reviewer, and Author Communities-April 2020.. 63:4409-4410. 2020
Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity.. 63:3298-3316. 2020
Cyanine-Gemcitabine Conjugates as Targeted Theranostic Agents for Glioblastoma Tumor Cells.. 62:9236-9245. 2019
Structure-Guided Drug Design of 6-Substituted Adenosine Analogues as Potent Inhibitors of Mycobacterium tuberculosis Adenosine Kinase.. 62:4483-4499. 2019
Application of Dually Activated Michael Acceptor to the Rational Design of Reversible Covalent Inhibitor for Enterovirus 71 3C Protease.. 62:6146-6162. 2019
Determination of Ligand Binding Epitope Structures Using Polarization Transfer from Hyperpolarized Ligands.. 62:2419-2427. 2019
Pyrimidinyl Biphenylureas: Identification of New Lead Compounds as Allosteric Modulators of the Cannabinoid Receptor CB1.. 60:1089-1104. 2017
New compstatin peptides containing N-terminal extensions and non-natural amino acids exhibit potent complement inhibition and improved solubility characteristics.. 58:814-826. 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
Optimization of chemical functionalities of indole-2-carboxamides to improve allosteric parameters for the cannabinoid receptor 1 (CB1).. 57:3040-3052. 2014
Structure-activity relationship study of indole-2-carboxamides identifies a potent allosteric modulator for the cannabinoid receptor 1 (CB1).. 56:7965-7975. 2013
Double-targeting using a TrkC ligand conjugated to dipyrrometheneboron difluoride (BODIPY) based photodynamic therapy (PDT) agent.. 56:7608-7614. 2013
Synthesis of new 7-oxycoumarin derivatives as potent and selective monoamine oxidase A inhibitors.. 55:10424-10436. 2012
In vitro and in vivo antitumor activities and DNA binding mode of five coordinated cyclometalated organoplatinum(II) complexes containing biphosphine ligands.. 54:6166-6176. 2011
Bivalent diketopiperazine-based tropomysin receptor kinase C (TrkC) antagonists.. 53:5044-5048. 2010
In vitro and in vivo photocytotoxicity of boron dipyrromethene derivatives for photodynamic therapy.. 53:2865-2874. 2010
Structural studies of pterin-based inhibitors of dihydropteroate synthase.. 53:166-177. 2010
Tea catechins inhibit hepatocyte growth factor receptor (MET kinase) activity in human colon cancer cells: kinetic and molecular docking studies.. 52:6543-6545. 2009
Magnetically aligned bicelles to study the orientation of lipophilic ligands in membrane bilayers.. 51:6793-6799. 2008
Bornyl- and isobornyl-Delta8-tetrahydrocannabinols: a novel class of cannabinergic ligands.. 51:6393-6399. 2008
Discovery of novel nitrobenzothiazole inhibitors for Mycobacterium tuberculosis ATP phosphoribosyl transferase (HisG) through virtual screening.. 51:5984-5992. 2008
N-substituted 3-acetyltetramic acid derivatives as antibacterial agents.. 51:1487-1491. 2008
Synthesis, stability, and antimicrobial studies of electronically tuned silver acetate N-heterocyclic carbenes.. 51:1577-1583. 2008
Cannabilactones: a novel class of CB2 selective agonists with peripheral analgesic activity.. 50:6493-6500. 2007
Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore.. 50:3777-3785. 2007
Synthesis and evaluation of 4/5-hydroxy-2,3-diaryl(substituted)-cyclopent-2-en-1-ones as cis-restricted analogues of combretastatin A-4 as novel anticancer agents.. 50:1744-1753. 2007
Dirhodium(II,II) complexes: molecular characteristics that affect in vitro activity.. 49:6841-6847. 2006
Synthesis from caffeine of a mixed N-heterocyclic carbene-silver acetate complex active against resistant respiratory pathogens.. 49:6811-6818. 2006
4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.. 48:5644-5647. 2005
Adamantyl cannabinoids: a novel class of cannabinergic ligands.. 48:4576-4585. 2005
Bisaryloxime ethers as potent inhibitors of transthyretin amyloid fibril formation.. 48:1576-1587. 2005
Diflunisal analogues stabilize the native state of transthyretin. Potent inhibition of amyloidogenesis.. 47:355-374. 2004
Molecular basis of neurotrophin-receptor interactions.. 46:5277-5291. 2003
Conformational study of lipophilic ligands in phospholipid model membrane systems by solution NMR.. 46:4838-4846. 2003
Selective formation of homo- and heterobivalent peptidomimetics.. 46:3565-3567. 2003
New templates for syntheses of ring-fused, C(10) beta-turn peptidomimetics leading to the first reported small-molecule mimic of neurotrophin-3.. 45:4387-4390. 2002
Synthesis and solution conformation of cyclo[RGDRGD]: a cyclic peptide with selectivity for the alpha V beta 3 receptor.. 39:4520-4526. 1996
Synthesis and structure-activity relationships of retinoid X receptor selective diaryl sulfide analogs of retinoic acid.. 39:3556-3563. 1996
Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells.. 38:3146-3155. 1995
Synthesis and structure-activity relationships of stilbene retinoid analogs substituted with heteroaromatic carboxylic acids.. 38:2820-2829. 1995
Combinatorial technologies involving reiterative division/coupling/recombination: statistical considerations.. 37:2985-2987. 1994
Rational design, synthesis, and crystallographic analysis of a hydroxyethylene-based HIV-1 protease inhibitor containing a heterocyclic P1'--P2' amide bond isostere.. 37:3100-3107. 1994
cis-4-Carboxy-6-(mercaptomethyl)-3,4,5,6-tetrahydropyrimidin-2(1 H)-one , a potent inhibitor of mammalian dihydroorotase.. 31:1355-1359. 1988
Prioritization of Eleven-Nineteen-Leukemia Inhibitors as Orally Available Drug Candidates for Acute Myeloid Leukemia.