Projects

Within the field of Drug Discovery, designing new scaffolds and easy accessible chemistry is very important. Through MCR Chemistry we try to develop druglike molecules in the following projects;

Scaffolds:

  • Recent Developments in Isocyanide Based Multicomponent Reactions in Applied Chemistry
  • The Gewald multicomponent reaction
  • Polycyclic Compounds by Ugi−Pictet−Spengler Sequence
  • Efficient Multicomponent Reaction Synthesis of the Schistosomiasis Drug Praziquantel
  • Cyanoacetamide MCR (III): Three-Component Gewald Reactions Revisited
  • One-pot Synthesis Of Highly Functionalized Seleno Aminoacid Derivatives
  • (-)Bacillamide C: The Convergent Approach

Medicinal Chemistry:

  • Parallel Synthesis Of Arrays Of 1,4,5-Trisubstituted 1-(4-Piperidyl)-Imidazoles By IMCR: A Novel Class Of Aspartyl Protease Inhibitors
  • Novel Anti-Tuberculosis Agents from MCR Libraries
  • One-Pot Synthesis of 2-Amino-indole-3-carboxamides
  • Praziquantel and Schistosomiasis

Protein Protein Interactions:

  • Small molecular weight protein-protein interaction antagonists: an insurmountable challenge?
  • Screening Multicomponent Reactions for X-Linked Inhibitor of Apoptosis-Baculoviral Inhibitor of Apoptosis Protein Repeats Domain Binder
  • Identification of Hsp70 modulators through modeling of the substrate binding domain
  • Towards Erythropoietin mimicking Small Molecules

p53 mdm2 mdm4:

  • Robust Generation of Lead Compounds for Protein–Protein Interactions by Computational and MCR Chemistry: p53/Hdm2 Antagonists
  • The Structure-Based Design of Mdm2/Mdmx–p53 Inhibitors Gets Serious
  • Structures of Low Molecular Weight Inhibitors Bound to MDMX and MDM2 Reveal New Approaches for p53-MDMX/MDM2 Antagonist Drug Discovery (open access)

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Chemistry in One Pot