All Stories

  1. Telomerase-based Cancer Therapeutics: A Review on their Clinical Trials
  2. A Jocic-type approach for a practical and scalable synthesis of pyrrolonaphthoxazepine (PNOX)-based potent proapoptotic agents
  3. Development of a Multiplexed Activity-Based Protein Profiling Assay to Evaluate Activity of Endocannabinoid Hydrolase Inhibitors
  4. Author Correction: The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity
  5. (S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation
  6. Activation of the Wnt Pathway by Small Peptides: Rational Design, Synthesis and Biological Evaluation
  7. The FAAH inhibitor URB597 suppresses hippocampal maximal dentate afterdischarges and restores seizure-induced impairment of short and long-term synaptic plasticity
  8. First dual AK/GSK-3β inhibitors endowed with antioxidant properties as multifunctional, potential neuroprotective agents
  9. Structural characterization of Giardia duodenalis thioredoxin reductase ( g TrxR) and computational analysis of its interaction with NBDHEX
  10. Computational Tool for Fast in silico Evaluation of hERG K+ Channel Affinity
  11. Identification of novel fluorescent probes preventing PrPSc replication in prion diseases
  12. Dopamine D3 Receptor Antagonists as Potential Therapeutics for the Treatment of Neurological Diseases
  13. Phenylpyrrole-based HDAC inhibitors: synthesis, molecular modeling and biological studies
  14. Development of novel cyclic peptides as pro-apoptotic agents
  15. Involvement of AMP-activated protein kinase in mediating pyrrolo-1,5-benzoxazepine–induced apoptosis in neuroblastoma cells
  16. Multiple Targeting Approaches on Histamine H3 Receptor Antagonists
  17. The pyrrolo-1,5-benzoxazepine, PBOX-15, enhances TRAIL-induced apoptosis by upregulation of DR5 and downregulation of core cell survival proteins in acute lymphoblastic leukaemia cells
  18. Polypharmacology of dopamine receptor ligands
  19. Targeting clinically-relevant metallo-β-lactamases: from high-throughput docking to broad-spectrum inhibitors
  20. Development and Pharmacological Characterization of Selective Blockers of 2-Arachidonoyl Glycerol Degradation with Efficacy in Rodent Models of Multiple Sclerosis and Pain
  21. In silico study of subtilisin-like protease 1 (SUB1) from different Plasmodium species in complex with peptidyl-difluorostatones and characterization of potent pan-SUB1 inhibitors
  22. The novel pyrrolo-1,5-benzoxazepine, PBOX-15, synergistically enhances the apoptotic efficacy of imatinib in gastrointestinal stromal tumours; suggested mechanism of action of PBOX-15
  23. Development of a practical and scalable route for the preparation of the deacetoxytubuvaline (dTuv) fragment of pretubulysin and analogs
  24. Multitarget compounds bearing tacrine- and donepezil-like structural and functional motifs for the potential treatment of Alzheimer's disease
  25. Harnessing the pyrroloquinoxaline scaffold for FAAH and MAGL interaction: definition of the structural determinants for enzyme inhibition
  26. Pre-clinical evaluation of a novel class of anti-cancer agents, the Pyrrolo-1, 5-benzoxazepines.
  27. Exploring clotrimazole-based pharmacophore: 3D-QSAR studies and synthesis of novel antiplasmodial agents
  28. Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation
  29. Antitumor effect of pyrrolo-1,5-benzoxazepine-15 and its synergistic effect with Oxaliplatin and 5-FU in colorectal cancer cells
  30. Site-directed Mutagenesis of Key Residues Unveiled a Novel Allosteric Site on Human Adenosine Kinase for Pyrrolobenzoxa(thia)zepinone Non-Nucleoside Inhibitors
  31. Endocannabinoid Modulation of Predator Stress-Induced Long-Term Anxiety in Rats
  32. Unconventional Knoevenagel-type indoles: Synthesis and cell-based studies for the identification of pro-apoptotic agents
  33. Induction of apoptosis in oral squamous carcinoma cells by pyrrolo-1,5-benzoxazepines
  34. Structure-based discovery of the first non-covalent inhibitors of Leishmania major tryparedoxin peroxidase by high throughput docking
  35. Development of HuperTacrines as Non-Toxic, Cholinesterase Inhibitors for the Potential Treatment of Alzheimer’s Disease
  36. Synthetic spirocyclic endoperoxides: new antimalarial scaffolds
  37. Plasmodium falciparum subtilisin-like protease 1: discovery of potent difluorostatone-based inhibitors
  38. Targeting Dopamine D 3 and Serotonin 5-HT 1A and 5-HT 2A Receptors for Developing Effective Antipsychotics: Synthesis, Biological Characterization, and Behavioral Studies
  39. Rational design of the first difluorostatone-based PfSUB1 inhibitors
  40. Disease-Modifying Anti-Alzheimer's Drugs: Inhibitors of Human Cholinesterases Interfering withβ-Amyloid Aggregation
  41. HCV-targeted Antivirals: Current Status and Future Challenges
  42. Retraction notice to “PBOX-15 induces apoptosis and improves the efficacy of oxaliplatin in human colorectal cancer cell lines” [Eur. J. Pharmacol. 714(1–3) (2013) 379–387]
  43. The novel pyrrolo-1,5-benzoxazepine, PBOX-6, synergistically enhances the apoptotic effects of carboplatin in drug sensitive and multidrug resistant neuroblastoma cells
  44. From (+)-epigallocatechin gallate to a simplified synthetic analogue as a cytoadherence inhibitor for P. falciparum
  45. Multifunctional Cholinesterase and Amyloid Beta Fibrillization Modulators. Synthesis and Biological Investigation
  46. A stereoselective approach to peptidomimetic BACE1 inhibitors
  47. A stereoselective route to 6-substituted pyrrolo-1,5-benzoxazepinones and their analogues
  48. RETRACTED: PBOX-15 induces apoptosis and improves the efficacy of oxaliplatin in human colorectal cancer cell lines
  49. The Structural Evolution of β-Secretase Inhibitors: A Focus on the Development of Small-Molecule Inhibitors
  50. Synthesis and structure–activity relationship studies in serotonin 5-HT1A receptor agonists based on fused pyrrolidone scaffolds
  51. A synthetic strategy to bridged 2,3,8-trioxabicyclo[3,3,1]nonane endoperoxides
  52. Novel peptidomimetics as BACE-1 inhibitors: Synthesis, molecular modeling, and biological studies
  53. Identification of a novel arylpiperazine scaffold for fatty acid amide hydrolase inhibition with improved drug disposition properties
  54. Mimicking the Intramolecular Hydrogen Bond: Synthesis, Biological Evaluation, and Molecular Modeling of Benzoxazines and Quinazolines as Potential Antimalarial Agents
  55. A Straightforward Approach for Engineering Efficacy and Selectivity at GPCRs
  56. Discovery of Potent Inhibitors of Human and Mouse Fatty Acid Amide Hydrolases
  57. Optimization of 4-Aminoquinoline/Clotrimazole-Based Hybrid Antimalarials: Further Structure–Activity Relationships, in Vivo Studies, and Preliminary Toxicity Profiling
  58. Quinolylhydrazones as novel inhibitors of Plasmodium falciparum serine protease PfSUB1
  59. The Ca2+-ATPase (SERCA1) Is Inhibited by 4-Aminoquinoline Derivatives through Interference with Catalytic Activation by Ca2+, Whereas the ATPase E2 State Remains Functional
  60. Synthesis and Antiplasmodial Activity of Bicyclic Dioxanes as Simplified Dihydroplakortin Analogues
  61. Selective Kainate Receptor (GluK1) Ligands Structurally Based upon 1 H -Cyclopentapyrimidin-2,4(1 H ,3 H )-dione: Synthesis, Molecular Modeling, and Pharmacological and Biostructural Characterization
  62. Enantioselective binding of second generation pyrrolobenzoxazepinones to the catalytic ternary complex of HIV-1 RT wild-type and L100I and K103N drug resistant mutants
  63. Discovery of potent nucleotide-mimicking competitive inhibitors of hepatitis C virus NS3 helicase
  64. Non-Nucleoside Inhibitors of Human Adenosine Kinase: Synthesis, Molecular Modeling, and Biological Studies
  65. Pyrroloquinoxaline hydrazones as fluorescent probes for amyloid fibrils
  66. PBOX-15, a novel microtubule targeting agent, induces apoptosis, upregulates death receptors and potentiates TRAIL-mediated apoptosis in multiple myeloma cells
  67. Malaria Chemotherapy: Recent Advances in Drug Development
  68. Discovery of Bishomo(hetero)arylpiperazines as Novel Multifunctional Ligands Targeting Dopamine D 3 and Serotonin 5-HT 1A and 5-HT 2A Receptors
  69. Synthesis of Dihydroplakortin, 6- epi -Dihydroplakortin, and Their C10-Desethyl Analogues
  70. The Interactions of the 5-HT3 Receptor with Quipazine-Like Arylpiperazine Ligands. The Journey Track at the End of the First Decade of the Third Millennium
  71. Inhibition of SERCA1 by a Novel Antimalarial Compound
  72. Novel, Potent, and Selective Quinoxaline-Based 5-HT 3 Receptor Ligands. 1. Further Structure−Activity Relationships and Pharmacological Characterization
  73. The Novel Tubulin-Targeting Agent Pyrrolo-1,5-Benzoxazepine-15 Induces Apoptosis in Poor Prognostic Subgroups of Chronic Lymphocytic Leukemia
  74. Synthetic studies toward 1,2-dioxanes as precursors of potential endoperoxide-containing antimalarials
  75. Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure–activity relationship studies
  76. Specific Targeting of Peripheral Serotonin 5-HT 3 Receptors. Synthesis, Biological Investigation, and Structure−Activity Relationships
  77. Specific Targeting of Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. 2. Stereoselective Interaction to Overcome the Effects of Drug Resistant Mutations
  78. The novel pyrrolo-1,5-benzoxazepine, PBOX-21, potentiates the apoptotic efficacy of STI571 (imatinib mesylate) in human chronic myeloid leukaemia cells
  79. Combining 4-Aminoquinoline- and Clotrimazole-Based Pharmacophores toward Innovative and Potent Hybrid Antimalarials
  80. Discovery of a New Class of Potential Multifunctional Atypical Antipsychotic Agents Targeting Dopamine D 3 and Serotonin 5-HT 1A and 5-HT 2A Receptors: Design, Synthesis, and Effects on Behavior
  81. An Efficient Approach to Chiral C8/C9-Piperazino-Substituted 1,4-Benzodiazepin-2-ones as Peptidomimetic Scaffolds
  82. 1 H -Cyclopentapyrimidine-2,4(1 H ,3 H )-dione-Related Ionotropic Glutamate Receptors Ligands. Structure−Activity Relationships and Identification of Potent and Selective iGluR5 Modulators
  83. Tacrine based human cholinesterase inhibitors: Synthesis of peptidic-tethered derivatives and their effect on potency and selectivity
  84. Selective targeting of the HIV-1 reverse transcriptase catalytic complex through interaction with the “primer grip” region by pyrrolobenzoxazepinone non-nucleoside inhibitors correlates with increased activity towards drug-resistant mutants
  85. Exploiting Protein Fluctuations at the Active-Site Gorge of Human Cholinesterases: Further Optimization of the Design Strategy to Develop Extremely Potent Inhibitors
  86. Microwave-assisted synthesis of 4-quinolylhydrazines followed by nickel boride reduction: a convenient approach to 4-aminoquinolines and derivatives
  87. Design, Synthesis, and Structure–Activity Relationship Studies of 4-Quinolinyl- and 9-Acrydinylhydrazones as Potent Antimalarial Agents
  88. Clotrimazole Scaffold as an Innovative Pharmacophore Towards Potent Antimalarial Agents: Design, Synthesis, and Biological and Structure–Activity Relationship Studies
  89. A new microtubule-targeting compound PBOX-15 inhibits T-cell migration via post-translational modifications of tubulin
  90. Development of piperazine-tethered heterodimers as potent antimalarials against chloroquine-resistant P. falciparum strains. Synthesis and molecular modeling
  91. Design and Synthesis of Potent Antimalarial Agents Based on Clotrimazole Scaffold:  Exploring an Innovative Pharmacophore
  92. Synthesis of N1-arylidene-N2-quinolyl- and N2-acrydinylhydrazones as potent antimalarial agents active against CQ-resistant P. falciparum strains
  93. Discovery of Huperzine A−Tacrine Hybrids as Potent Inhibitors of Human Cholinesterases Targeting Their Midgorge Recognition Sites
  94. Specific Targeting Highly Conserved Residues in the HIV-1 Reverse Transcriptase Primer Grip Region. Design, Synthesis, and Biological Evaluation of Novel, Potent, and Broad Spectrum NNRTIs with Antiviral Activity
  95. Specific Targeting of Hepatitis C Virus NS3 RNA Helicase. Discovery of the Potent and Selective Competitive Nucleotide-Mimicking Inhibitor QU663 †
  96. Pyrrolo[1,5]benzoxa(thia)zepines as a New Class of Potent Apoptotic Agents. Biological Studies and Identification of an Intracellular Location of Their Drug Target
  97. Development of Molecular Probes for the Identification of Extra Interaction Sites in the Mid-Gorge and Peripheral Sites of Butyrylcholinesterase (BuChE). Rational Design of Novel, Selective, and Highly Potent BuChE Inhibitors †
  98. Novel Atypical Antipsychotic Agents:  Rational Design, an Efficient Palladium-Catalyzed Route, and Pharmacological Studies
  99. Pyrrolo[1,3]benzothiazepine-Based Serotonin and Dopamine Receptor Antagonists. Molecular Modeling, Further Structure−Activity Relationship Studies, and Identification of Novel Atypical Antipsychotic Agents
  100. Synthesis and Pharmacological Evaluation of Potent and Highly Selective D 3 Receptor Ligands:  Inhibition of Cocaine-Seeking Behavior and the Role of Dopamine D 3 /D 2 Receptors †
  101. A Palladium-Catalyzed Synthetic Approach to New Huperzine A Analogues Modified at the Pyridone Ring.
  102. Novel antipsychotic agents: recent advances in the drug treatment of schizophrenia
  103. Neuronal High-Affinity Sodium-Dependent Glutamate Transporters (EAATs): Targets for the Development of Novel Therapeutics Against Neurodegenerative Diseases
  104. A palladium-catalyzed synthetic approach to new Huperzine A analogues modified at the pyridone ring
  105. Novel antipsychotic agents: recent advances in the drug treatment of schizophrenia
  106. Polycondensed heterocycles. Part 12: An approach to the synthesis of 2-acetyl-1′-methyl-1,2,3,4-tetrahydrospiro[isoquinoline-1,4′-pyrrolidine]-2′-one
  107. Pyrrolo[1,3]benzothiazepine-Based Atypical Antipsychotic Agents. Synthesis, Structure−Activity Relationship, Molecular Modeling, and Biological Studies
  108. Pyrroloquinoxaline Derivatives as High-Affinity and Selective 5-HT 3 Receptor Agonists:  Synthesis, Further Structure−Activity Relationships, and Biological Studies