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)