Journal of medicinal chemistry

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Lead Optimization of Androgen Receptor-HSP27 Disrupting Agents in Glioblastoma.. 66. 2023
Structure-Activity Relationship Studies of Antimalarial Plasmodium Proteasome Inhibitors─Part II.. 66. 2023
Discovery of Highly Selective Inhibitors of the Human Constitutive Proteasome β5c Chymotryptic Subunit.. 66. 2023
Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates.. 65. 2022
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.. 65. 2022
Design, Synthesis, and Optimization of Macrocyclic Peptides as Species-Selective Antimalaria Proteasome Inhibitors.. 65. 2022
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.. 65. 2022
In Vitro and In Vivo Inhibition of the Mycobacterium tuberculosis Phosphopantetheinyl Transferase PptT by Amidinoureas.. 65. 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. 2021
Macrocyclic Peptides that Selectively Inhibit the Mycobacterium tuberculosis Proteasome.. 64. 2021
Progress toward B-Cell Lymphoma 6 BTB Domain Inhibitors for the Treatment of Diffuse Large B-Cell Lymphoma and Beyond.. 64. 2021
Small-Molecule HSP27 Inhibitor Abolishes Androgen Receptors in Glioblastoma.. 64. 2021
Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies.. 64. 2021
Saturated Hydroxy Fatty Acids Exhibit a Cell Growth Inhibitory Activity and Suppress the Cytokine-Induced β-Cell Apoptosis.. 63. 2020
Structure-Activity Relationships of Noncovalent Immunoproteasome β5i-Selective Dipeptides.. 63. 2020
Assessing the Perturbing Effects of Drugs on Lipid Bilayers Using Gramicidin Channel-Based In Silico and In Vitro Assays.. 63. 2020
MicroRNA-Based Multitarget Approach for Alzheimer's Disease: Discovery of the First-In-Class Dual Inhibitor of Acetylcholinesterase and MicroRNA-15b Biogenesis.. 63. 2020
Novel, Self-Assembling Dimeric Inhibitors of Human β Tryptase.. 63. 2020
Selective Phenylimidazole-Based Inhibitors of the Mycobacterium tuberculosis Proteasome.. 62. 2019
Improvement of Asparagine Ethylenediamines as Anti-malarial Plasmodium-Selective Proteasome Inhibitors.. 62. 2019
Novel Lysine-Based Thioureas as Mechanism-Based Inhibitors of Sirtuin 2 (SIRT2) with Anticancer Activity in a Colorectal Cancer Murine Model.. 62. 2019
Development of Gleevec Analogues for Reducing Production of β-Amyloid Peptides through Shifting β-Cleavage of Amyloid Precursor Proteins.. 62. 2019
Photoactivatable Prodrug of Doxazolidine Targeting Exosomes.. 62. 2019
Discovery and Structure-Activity-Relationship Study of N-Alkyl-5-hydroxypyrimidinone Carboxamides as Novel Antitubercular Agents Targeting Decaprenylphosphoryl-β-d-ribose 2'-Oxidase.. 61. 2018
Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.. 61. 2018
Identification of Thiourea-Based Inhibitors of the B-Cell Lymphoma 6 BTB Domain via NMR-Based Fragment Screening and Computer-Aided Drug Design.. 61. 2018
¹⁸F-Positron Emitting/Trimethine Cyanine-Fluorescent Contrast for Image-Guided Prostate Cancer Management.. 61. 2018
Exploring Structural Parameters for Pretargeting Radioligand Optimization.. 60. 2017
Structure-Based Optimization of Pyridoxal 5'-Phosphate-Dependent Transaminase Enzyme (BioA) Inhibitors that Target Biotin Biosynthesis in Mycobacterium tuberculosis.. 60. 2017
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.. 59. 2016
Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity.. 59. 2016
Targeting Mycobacterium tuberculosis Biotin Protein Ligase (MtBPL) with Nucleoside-Based Bisubstrate Adenylation Inhibitors.. 58. 2015
Discovery of a Novel Class of Negative Allosteric Modulator of the Dopamine D2 Receptor Through Fragmentation of a Bitopic Ligand.. 58. 2015
Fragment-based exploration of binding site flexibility in Mycobacterium tuberculosis BioA.. 58. 2015
Detailed Biological Profiling of a Photoactivated and Apoptosis Inducing pdppz Ruthenium(II) Polypyridyl Complex in Cancer Cells.. 58. 2015
CB2-selective cannabinoid receptor ligands: synthesis, pharmacological evaluation, and molecular modeling investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides.. 57. 2014
Design, synthesis, structure-function relationship, bioconversion, and pharmacokinetic evaluation of ertapenem prodrugs.. 57. 2014
Radioiodinated benzyloxybenzene derivatives: a class of flexible ligands target to β-amyloid plaques in Alzheimer's brains.. 57. 2014
Alternative chelator for ⁸⁹Zr radiopharmaceuticals: radiolabeling and evaluation of 3,4,3-(LI-1,2-HOPO).. 57. 2014
Synthetic calanolides with bactericidal activity against replicating and nonreplicating Mycobacterium tuberculosis.. 57. 2014
Heat shock protein 70 inhibitors. 1. 2,5'-thiodipyrimidine and 5-(phenylthio)pyrimidine acrylamides as irreversible binders to an allosteric site on heat shock protein 70.. 57. 2014
Heat shock protein 70 inhibitors. 2. 2,5'-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70.. 57. 2014
Elucidation of structural elements for selectivity across monoamine transporters: novel 2-[(diphenylmethyl)sulfinyl]acetamide (modafinil) analogues.. 57. 2014
Synthesis and anticancer mechanism investigation of dual Hsp27 and tubulin inhibitors.. 56. 2013
Synthesis and SAR of novel Re/99mTc-labeled benzenesulfonamide carbonic anhydrase IX inhibitors for molecular imaging of tumor hypoxia.. 56. 2013
Novel cyclopentadienyl tricarbonyl complexes of (99m)Tc mimicking chalcone as potential single-photon emission computed tomography imaging probes for β-amyloid plaques in brain.. 56. 2013
Synthesis and evaluation of novel ¹⁸F labeled 2-pyridinylbenzoxazole and 2-pyridinylbenzothiazole derivatives as ligands for positron emission tomography (PET) imaging of β-amyloid plaques.. 55. 2012
Design, synthesis, and biological and structural evaluations of novel HIV-1 protease inhibitors to combat drug resistance.. 55. 2012
Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.. 55. 2012
Identification of a class of novel tubulin inhibitors.. 55. 2012
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.. 54. 2011
Synthesis and evaluation of radioligands for imaging brain nociceptin/orphanin FQ peptide (NOP) receptors with positron emission tomography.. 54. 2011
Role of metalation in the topoisomerase IIα inhibition and antiproliferation activity of a series of α-heterocyclic-N4-substituted thiosemicarbazones and their Cu(II) complexes.. 54. 2011
Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands.. 54. 2010
Thiadiazole carbamates: potent inhibitors of lysosomal acid lipase and potential Niemann-Pick type C disease therapeutics.. 53. 2010
Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).. 53. 2010
Synthesis and characterization of rhenium and technetium-99m labeled insulin.. 53. 2010
Design and synthesis of novel diaminoquinazolines with in vivo efficacy for beta-catenin/T-cell transcriptional factor 4 pathway inhibition.. 53. 2010
Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent.. 52. 2009
Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.. 52. 2009
Discovery of potent and selective inhibitors of the mammalian target of rapamycin (mTOR) kinase.. 52. 2009
Investigation of N-aryl-3-alkylidenepyrrolinones as potential Niemann-Pick type C disease therapeutics.. 52. 2009
Nitazoxanide kills replicating and nonreplicating Mycobacterium tuberculosis and evades resistance.. 52. 2009
ATP-competitive inhibitors of the mammalian target of rapamycin: design and synthesis of highly potent and selective pyrazolopyrimidines.. 52. 2009
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.. 52. 2009
Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus with a reduced potential to increase plasma and extracellular fluid volume.. 52. 2009
Discovery of the development candidate N-tert-butyl nodulisporamide: a safe and efficacious once monthly oral agent for the control of fleas and ticks on companion animals.. 52. 2009
Single-step high-yield radiosynthesis and evaluation of a sensitive 18F-labeled ligand for imaging brain peripheral benzodiazepine receptors with PET.. 52. 2009
A series of halogenated heterodimeric inhibitors of prostate specific membrane antigen (PSMA) as radiolabeled probes for targeting prostate cancer.. 52. 2009
Radiohalogenated prostate-specific membrane antigen (PSMA)-based ureas as imaging agents for prostate cancer.. 51. 2008
Alteration of the bis-tetrahydrofuran core stereochemistries in asimicin can affect the cytotoxicity.. 51. 2008
Novel microtubule-interacting phenoxy pyridine and phenyl sulfanyl pyridine analogues for cancer therapy.. 51. 2008
Structure-based development of novel adenylyl cyclase inhibitors.. 51. 2008
In vitro and in vivo evaluation of bifunctional bisthiosemicarbazone 64Cu-complexes for the positron emission tomography imaging of hypoxia.. 51. 2008
Synthesis and evaluation in monkey of two sensitive 11C-labeled aryloxyanilide ligands for imaging brain peripheral benzodiazepine receptors in vivo.. 51. 2007
Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.. 50. 2007
Identification of anthranilic acid derivatives as a novel class of allosteric inhibitors of hepatitis C NS5B polymerase.. 50. 2007
Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues.. 50. 2007
Synthesis and evaluation of [18F] labeled pyrimidine nucleosides for positron emission tomography imaging of herpes simplex virus 1 thymidine kinase gene expression.. 49. 2006
Validation of a novel CHX-A'' derivative suitable for peptide conjugation: small animal PET/CT imaging using yttrium-86-CHX-A''-octreotide.. 49. 2006
Discovery of proline sulfonamides as potent and selective hepatitis C virus NS5b polymerase inhibitors. Evidence for a new NS5b polymerase binding site.. 49. 2006
Benzoylphenylurea sulfur analogues with potent antitumor activity.. 49. 2006
Novel 2,3-dihydrobenzofuran-2-carboxylic acids: highly potent and subtype-selective PPARalpha agonists with potent hypolipidemic activity.. 48. 2005
Evaluation of 8-arylsulfanyl, 8-arylsulfoxyl, and 8-arylsulfonyl adenine derivatives as inhibitors of the heat shock protein 90.. 48. 2005
Imaging of melanoma using 64Cu- and 86Y-DOTA-ReCCMSH(Arg11), a cyclized peptide analogue of alpha-MSH.. 48. 2005
Chemical adaptor immunotherapy: design, synthesis, and evaluation of novel integrin-targeting devices.. 47. 2004
Synthesis of flexible sulfur-containing heteroarotinoids that induce apoptosis and reactive oxygen species with discrimination between malignant and benign cells.. 47. 2004
Neuromuscular blocking activity and therapeutic potential of mixed-tetrahydroisoquinolinium halofumarates and halosuccinates in rhesus monkeys.. 46. 2003
In vitro and in vivo antitumor properties of tetrakis((trishydroxy- methyl)phosphine)gold(I) chloride.. 46. 2003
Synthesis of apicidin-derived quinolone derivatives: parasite-selective histone deacetylase inhibitors and antiproliferative agents.. 43. 2000
Comparison of four 64Cu-labeled somatostatin analogues in vitro and in a tumor-bearing rat model: evaluation of new derivatives for positron emission tomography imaging and targeted radiotherapy.. 42. 1999
Bis- and mixed-tetrahydroisoquinolinium chlorofumarates: new ultra-short-acting nondepolarizing neuromuscular blockers.. 42. 1999
Synthesis and biological evaluation of 2-acyl analogues of paclitaxel (Taxol).. 41. 1998
Signal transduction by a 5-HT2 receptor: a mechanistic hypothesis from molecular dynamics simulations of the three-dimensional model of the receptor complexed to ligands.. 36. 1993
Affinity probes for the avermectin binding proteins.. 35. 1992
Synthesis and calcium channel antagonist activity of dialkyl 4- (dihydropyridinyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinecarboxylates.. 30. 1987
Synthesis and calcium channel antagonist activity of dialkyl 1,4-dihydro-2,6-dimethyl-4-(pyridinyl)-3,5-pyridinedicarboxylates.. 29. 1986
Molecular determinants for the agonist activity of 2-methylhistamine and 4-methylhistamine at H2-receptors.. 29. 1986
Improved synthesis of 2'-deoxyformycin A and studies of its in vitro activity against mouse lymphoma of T-cell origin.. 28. 1985
A theoretical investigation of histamine tautomerism.. 27. 1984
Synthesis of alpha-1-noracetylmethadol. A facile N-demethylation of alpha-1-acetylmethadol.. 18. 1975
Stereospecific synthesis of the 6beta-hydroxy metabolites of naltrexone and naloxone.. 18. 1975
Rational approaches to improving selectivity in drug design. 2012
Perspectives in animal health: old targets and new opportunities. 2001

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