All Stories

  1. Gold Nanostars Bioconjugation for Selective Targeting and SERS Detection of Biofluids
  2. Multitargeting application of proline-derived peptidomimetics addressing cancer-related human matrix metalloproteinase 9 and carbonic anhydrase II
  3. Occurrence of Morpholine in Central Nervous System Drug Discovery
  4. Discovery of a d-pro-lys peptidomimetic inhibitor of MMP9: Addressing the gelatinase selectivity beyond S1′ subsite
  5. Recent advances in copper-catalyzed imine-based multicomponent reactions
  6. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–7
  7. A Glucose‐Derived α‐Hydroxy Aldehyde for the Petasis Reaction: Facile Access to Polyfunctional δ‐Amino Acids
  8. Nanostars—decorated microfluidic sensors for surface enhanced Raman scattering targeting of biomolecules
  9. Combination of multicomponent KA2 and Pauson–Khand reactions: short synthesis of spirocyclic pyrrolocyclopentenones
  10. Peptidomimetic toolbox for drug discovery
  11. Breakthroughs in Medicinal Chemistry: New Targets and Mechanisms, New Drugs, New Hopes–6
  12. Copper-Catalyzed A3 -Coupling for the Diversity-Oriented Synthesis of Proline-Derived Alkynyl-Substituted Peptidomimetic Scaffolds
  13. Identification of highly potent and selective MMP2 inhibitors addressing the S1′ subsite with d-proline-based compounds
  14. Occurrence of the d-Proline Chemotype in Enzyme Inhibitors
  15. Smart Design of Small‐Molecule Libraries: When Organic Synthesis Meets Cheminformatics
  16. Bicyclic acetals: biological relevance, scaffold analysis, and applications in diversity-oriented synthesis
  17. Exploring the chemical space and the bioactivity profile of lactams: a chemoinformatic study
  18. Deciphering the mechanism of action of 089, a compound impairing the fungal cell cycle
  19. Dual Iminium- and Lewis Base Catalyzed Morita–Baylis–Hillman Reaction on Cyclopent-2-enone
  20. Corrigendum to “Design and synthesis of bicyclic acetals as Beta Secretase (BACE1) inhibitors” [Bioorg. Med. Chem. 25 (2017) 5077–5083]
  21. Design and synthesis of bicyclic acetals as Beta Secretase (BACE1) inhibitors
  22. Design and synthesis of bioactive compounds
  23. Relations between Effects and Structure of Small Bicyclic Molecules on the Complex Model System Saccharomyces cerevisiae
  24. Short synthesis of polyfunctional sp3-rich threonine-derived morpholine scaffolds
  25. Identification of Novel Human Breast Carcinoma (MDA-MB-231) Cell Growth Modulators from a Carbohydrate-Based Diversity Oriented Synthesis Library
  26. Triazole RGD antagonist reverts TGFβ1-induced endothelial-to-mesenchymal transition in endothelial precursor cells
  27. Insight to the binding mode of triazole RGD-peptidomimetics to integrin-rich cancer cells by NMR and molecular modeling
  28. Cyclic RGD peptidomimetics containing 4- and 5-amino-cyclopropane pipecolic acid (CPA) templates as dual αVβ3 and α5β1 integrin ligands
  29. Carbohydrates in diversity-oriented synthesis: challenges and opportunities
  30. Radiosynthesis and micro-SPECT analysis of triazole-based RGD integrin ligands as non-peptide molecular imaging probes for angiogenesis
  31. Skeletal Diversity from Carbohydrates: Use of Mannose for the Diversity-Oriented Synthesis of Polyhydroxylated Compounds
  32. A study of ad-proline peptidomimetic inhibitor of melanoma and endothelial cell invasion through activity towards MMP-2 and MMP-9
  33. Two-step one-pot synthesis of dihydropyrazinones as Xaa-Ser dipeptide isosteres through morpholine acetal rearrangement
  34. Role of Side-Chain Bioisosteres in Determining the Binding Affinity of Click Chemistry Derived RGD Peptidomimetics to αvβ3Integrin
  35. Diversity-Oriented Synthesis as a Tool for Chemical Genetics
  36. Peptidomimetics as protein arginine deiminase 4 (PAD4) inhibitors
  37. Identification of constrained peptidomimetic chemotypes as HIV protease inhibitors
  38. Combination of click chemistry and sulfonamides to develop three-armed triazole compounds
  39. Cyclopropane Pipecolic Acids as Templates for Linear and Cyclic Peptidomimetics: Application in the Synthesis of an Arg-Gly-Asp (RGD)-Containing Peptide as an αvβ3Integrin Ligand
  40. Use of Click-Chemistry in the Development of Peptidomimetic Enzyme Inhibitors
  41. Evaluation of efficacy, pharmacokinetics and tolerability of peptidomimetic aspartic proteinase inhibitors as cream formulation in experimental vaginal candidiasis
  42. Peptidomimetics in Organic and Medicinal Chemistry
  43. Heterocyclic HIV-Protease Inhibitors
  44. Diversity-Oriented Synthesis
  45. Diversity-Oriented Synthesis of Amino Acid-Derived Scaffolds and Peptidomimetics: A Perspective
  46. Bicyclic peptidomimetics targeting secreted aspartic protease 2 (SAP2) from Candida albicans reveal a constrained inhibitory chemotype
  47. Synthesis and conformational studies of a hybrid β-alanine–morpholine tetramer
  48. d-Proline-based peptidomimetic inhibitors of anthrax lethal factor
  49. Insight into the structural similarity between HIV protease and secreted aspartic protease-2 and binding mode analysis of HIV-Candida albicansinhibitors
  50. 125I-Radiolabeled Morpholine-Containing Arginine–Glycine–Aspartate (RGD) Ligand of αvβ3 Integrin As a Molecular Imaging Probe for Angiogenesis
  51. One-pot sequential Ti-/Cu-catalysis for tandem amidation/Ullmann-type cyclization: synthesis of model benzodiazepine(di)ones promoted by microwave irradiation
  52. Synthesis of diverse phenylglycine derivatives via transformation of Ugi four-component condensation primary adducts
  53. A New Family of Cinchona-Derived Amino Phosphine Precatalysts: Application to the Highly Enantio- and Diastereoselective Silver-Catalyzed Isocyanoacetate Aldol Reaction
  54. Novel small molecules for the treatment of infections caused byCandida albicans: a patent review (2002 – 2010)
  55. Chemical genetics approach to drug discovery by diversity-oriented synthesis (DOS) of peptidomimetics
  56. Skeletal diversity by sequential one-pot and stepwise routes using morpholine ester scaffolds
  57. Click-Chemistry-Derived Triazole Ligands of Arginine−Glycine−Aspartate (RGD) Integrins with a Broad Capacity To Inhibit Adhesion of Melanoma Cells and Both in Vitro and in Vivo Angiogenesis
  58. A Systems Biology Approach to Dissection of the Effects of Small Bicyclic Peptidomimetics on a Panel of Saccharomyces cerevisiae Mutants
  59. Identification of Inhibitors of Drug-Resistant Candida albicans Strains from a Library of Bicyclic Peptidomimetic Compounds
  60. Chemical genetics approach to identify new small molecule modulators of cell growth by phenotypic screening of Saccharomyces cerevisiae strains with a library of morpholine-derived compounds
  61. Evaluation of stereochemically dense morpholine-based scaffolds as proline surrogates in β-turn peptides
  62. Synthesis of γ‐ and δ‐Amino Acids
  63. Diversity-Oriented Synthesis of Morpholine-Containing Molecular Scaffolds
  64. Configurationally driven folding of model tetrapeptides containing L- or D-morpholine-3-carboxylic acids as β-turn nucleators
  65. Cyclic DGR-peptidomimetic containing a bicyclic reverse turn inducer as a selective αvβ5 integrin ligand
  66. Synthesis of cyclic peptide as a potent integrin ligand targeting angiogenesis
  67. Dimethoxyacetaldehyde
  68. Synthesis of a bicyclic δ-amino acid as a constrained Gly-Asn dipeptide isostere
  69. Stereoselective cyclopropanation of serine- and threonine-derived oxazines to access new morpholine-based scaffolds
  70. LiNTf 2 -Catalyzed Aminolysis of Lactones with Stoichiometric Quantities of Amines
  71. Diastereoselective Synthesis of Highly Constrained Spiro-β-Lactams by the Staudinger Reaction Using an Unsymmetrical Bicyclic Ketene
  72. Structural diversity of bicyclic amino acids
  73. Convenient Route to Enantiopure Fmoc-Protected Morpholine-3-carboxylic Acid
  74. Synthesis and Conformational Analysis of Constrained β-Turn Mimetics Incorporating a Bicyclic Turn Inducer by Use of the Petasis Three-Component Reaction on Solid Phase
  75. Synthesis of a Bicyclic Proline Analogue from l -Ascorbic Acid
  76. 3-Aza-6,8-dioxabicyclo[3.2.1]octanes as new enantiopure heteroatom-rich tropane-like ligands of human dopamine transporter
  77. 3-Aza-8,10-dioxa-bicyclo[5.2.1]decane (9-exo BTKa) carboxylic acid as a new reverse turn inducer: synthesis and conformational analysis of a model peptide
  78. Design, Synthesis, and Applications of 3-Aza-6,8-Dioxabicyclo[3.2.1]Octane-Based Scaffolds for Peptidomimetic Chemistry
  79. Synthesis of a constrained tricyclic scaffold based on trans-4-hydroxy-l-proline
  80. Synthesis of Glycidol- and Sugar-Derived Bicyclic β- and γ/δ-Amino Acids for Peptidomimetic Design
  81. γ- and δ-Amino Acids: Synthetic Strategies and Relevant Applications
  82. Solvent-Dependent Conformational Behaviour of Model Tetrapeptides Containing a Bicyclic Proline Mimetic
  83. Enantiospecific synthesis of 3-aza-6,8-dioxa-bicyclo[3.2.1]octane carboxylic acids from erythrose
  84. A new bicyclic proline-mimetic amino acid
  85. Synthesis of a new enantiopure bicyclic γ/δ-amino acid (BTKa) derived from tartaric acid and α-amino acetophenone
  86. Synthesis and Conformational Analysis of Small Peptides Containing 6-Endo-BT(t)L Scaffolds as Reverse Turn Mimetics
  87. Effect of C-ring modifications in benzo[c]quinolizin-3-ones, new selective inhibitors of human 5α-reductase 1
  88. Introduction of the new dipeptide isostere 7-endo-BtA as reverse turn inducer in a Bowman-Birk proteinase inhibitor
  89. Suzuki Reaction of Vinyl Triflates from Six- and Seven-Membered N-Alkoxycarbonyl Lactams with Boronic Acids and Esters
  90. Pd(0)-Catalyzed Cross-Coupling Reactions of Boron Derivatives with a Lactam-Derived N-Boc Enol Triflate
  91. A solid-phase approach towards the development of 3-aza-6,8-dioxabicyclo[3.2.1]octane scaffolds
  92. Synthesis and Reactivity of Bicycles Derived from Tartaric Acid and α-Amino Acids:  A Novel Class of Conformationally Constrained Dipeptide Isosteres Based upon Enantiopure 3-Aza-6,8-dioxabicyclo[3.2.1]octane-7-carboxylic Acid