Journal of Medicinal Chemistry

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  Publication Venue For

  • Structure-Guided Discovery of Potent Antifungals that Prevent Ras Signaling by Inhibiting Protein Farnesyltransferase..  65:13753-13770. 2022
  • Mechanistic Investigation of Site-specific DNA Methylating Agents Targeting Breast Cancer Cells..  64:12651-12669. 2021
  • Design, Synthesis, and Mechanism Study of Benzenesulfonamide-Containing Phenylalanine Derivatives as Novel HIV-1 Capsid Inhibitors with Improved Antiviral Activities..  63:4790-4810. 2020
  • Synthesis and Biological Evaluation of Subglutinol Analogs for Immunomodulatory Agents..  63:283-294. 2020
  • Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators..  62:8357-8363. 2019
  • Synthesis and Structure-Activity Relationship Correlations of Gnidimacrin Derivatives as Potent HIV-1 Inhibitors and HIV Latency Reversing Agents..  62:6958-6971. 2019
  • D2 Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine..  62:4755-4771. 2019
  • Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties..  62:1484-1501. 2019
  • Synthetic HIV V3 Glycopeptide Immunogen Carrying a N334 N-Glycan Induces Glycan-Dependent Antibodies with Promiscuous Site Recognition..  61:10116-10125. 2018
  • Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia..  61:4348-4369. 2018
  • Discovery of LSZ102, a Potent, Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen Receptor Positive Breast Cancer..  61:2837-2864. 2018
  • Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors..  60:6678-6692. 2017
  • Discovery of an Acrylic Acid Based Tetrahydroisoquinoline as an Orally Bioavailable Selective Estrogen Receptor Degrader for ERα+ Breast Cancer..  60:2790-2818. 2017
  • Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers..  59:9173-9200. 2016
  • Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1..  59:9262-9268. 2016
  • Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177)..  59:7915-7935. 2016
  • Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus..  59:3689-3704. 2016
  • Structure-Activity Relationship Studies of Mitogen Activated Protein Kinase Interacting Kinase (MNK) 1 and 2 and BCR-ABL1 Inhibitors Targeting Chronic Myeloid Leukemic Cells..  59:3063-3078. 2016
  • Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models..  59:578-591. 2016
  • Optimization of a Novel Series of Ataxia-Telangiectasia Mutated Kinase Inhibitors as Potential Radiosensitizing Agents..  59:559-577. 2016
  • Gnidimacrin, a Potent Anti-HIV Diterpene, Can Eliminate Latent HIV-1 Ex Vivo by Activation of Protein Kinase C β..  58:8638-8646. 2015
  • Synthesis and Biological Evaluation of Manassantin Analogues for Hypoxia-Inducible Factor 1α Inhibition..  58:7659-7671. 2015
  • Discovery and Optimization of a Porcupine Inhibitor..  58:5889-5899. 2015
  • Oral Selective Estrogen Receptor Downregulators (SERDs), a Breakthrough Endocrine Therapy for Breast Cancer..  58:4883-4887. 2015
  • Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents..  58:1992-2002. 2015
  • Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands..  56:8404-8421. 2013
  • Synthesis, structure, and antibiotic activity of aryl-substituted LpxC inhibitors..  56:6954-6966. 2013
  • Interfacial cavity filling to optimize CD4-mimetic miniprotein interactions with HIV-1 surface glycoprotein..  56:5033-5047. 2013
  • Novel adamantyl cannabinoids as CB1 receptor probes..  56:3904-3921. 2013
  • Chemistry and pharmacological studies of 3-alkoxy-2,5-disubstituted-pyridinyl compounds as novel selective α4β2 nicotinic acetylcholine receptor ligands that reduce alcohol intake in rats..  56:3000-3011. 2013
  • New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1..  56:2029-2037. 2013
  • Anti-AIDS agents 90. novel C-28 modified bevirimat analogues as potent HIV maturation inhibitors..  55:8128-8136. 2012
  • Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates..  55:7219-7229. 2012
  • Structure-functional selectivity relationship studies of β-arrestin-biased dopamine D₂ receptor agonists..  55:7141-7153. 2012
  • Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors..  53:8287-8297. 2010
  • Amino derivatives of indole as potent inhibitors of isoprenylcysteine carboxyl methyltransferase..  53:6838-6850. 2010
  • Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents..  53:6867-6888. 2010
  • Diarylaniline derivatives as a distinct class of HIV-1 non-nucleoside reverse transcriptase inhibitors..  53:4906-4916. 2010
  • Identification and functional characterization of a stable, centrally active derivative of the neurotensin (8-13) fragment as a potential first-in-class analgesic..  53:4623-4632. 2010
  • Anti-AIDS agents 81. Design, synthesis, and structure-activity relationship study of betulinic acid and moronic acid derivatives as potent HIV maturation inhibitors..  53:3133-3141. 2010
  • Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors..  52:7887-7891. 2009
  • High lipophilicity of meta Mn(III) N-alkylpyridylporphyrin-based superoxide dismutase mimics compensates for their lower antioxidant potency and makes them as effective as ortho analogues in protecting superoxide dismutase-deficient Escherichia coli..  52:7868-7872. 2009
  • Discovery of geranylgeranyltransferase-I inhibitors with novel scaffolds by the means of quantitative structure-activity relationship modeling, virtual screening, and experimental validation..  52:4210-4220. 2009
  • Heterobiaryl human immunodeficiency virus entry inhibitors..  52:4481-4487. 2009
  • Anti-AIDS agents. 78. Design, synthesis, metabolic stability assessment, and antiviral evaluation of novel betulinic acid derivatives as potent anti-human immunodeficiency virus (HIV) agents..  52:3248-3258. 2009
  • Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors..  51:6642-6645. 2008
  • Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists..  51:5506-5521. 2008
  • Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor..  51:4632-4640. 2008
  • Anti-tumor Activity of S-(p-bromobenzyl)glutathione Diesters in vitro: a Structure-Activity Study.  39:3409-3411. 1996