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Related Experiment Videos

Bifunctional scaffolds as templates for synthetic combinatorial libraries

V Krchnák1, A S Weichsel, O Issakova

  • 1Selectide Corporation, Hoechst Marion Roussel, Tucson, AZ 85737, USA.

Molecular Diversity
|May 1, 1996
PubMed
Summary

Researchers developed a diverse small-molecule library for drug discovery. This library successfully identified specific binders for streptavidin, demonstrating its potential in identifying novel therapeutic compounds.

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Area of Science:

  • Medicinal Chemistry
  • Synthetic Chemistry
  • Biotechnology

Background:

  • Combinatorial chemistry enables the rapid synthesis of large compound libraries.
  • Small cyclic scaffolds are valuable frameworks for designing potential drug candidates.
  • Identifying specific binders to protein targets is crucial for drug discovery.

Purpose of the Study:

  • To design and synthesize a novel small-molecule combinatorial library.
  • To explore the utility of this library in identifying specific binders to a model target.
  • To establish a method for structure determination of active compounds.

Main Methods:

  • A combinatorial library was synthesized using 20 amino acids, 10 aromatic hydroxy acids, and 21 alcohols.
  • Mitsunobu polymer-supported etherification was employed for the final randomization step.

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  • On-bead and in-solution screening methods were utilized, with compounds linked to beads via ester bonds.

    • Main Results:

    • A library of 4200 unique compounds was generated.
    • Specific binders to streptavidin were identified from the synthesized library.
    • The structures of the most active compounds were elucidated using MS/MS fragmentation analysis.

    Conclusions:

    • The developed combinatorial library is effective in identifying specific binders.
    • The synthetic strategy allows for rapid generation of diverse small molecules with potential pharmacophores.
    • This approach is valuable for hit identification in drug discovery programs.