Grafting a chromophore on AMD070 analogues for CXCR4 bioimaging: Chemical synthesis and in vitro assessment of the inhibition properties of the CXCR4 receptor

Bioorg Med Chem Lett. 2025 Jan 1:115:130027. doi: 10.1016/j.bmcl.2024.130027. Epub 2024 Nov 17.

Abstract

Thank to their particular pharmacokinetics, the use of small organic molecules can be a very promising alternative to macromolecular targeting biomolecules (i.e. antibodies, peptides…) for specific imaging of tumours. Herein, the potential of two AMD070-like inhibitors as CXCR4-targeting units for specific imaging of cancer cells, and the influence of chromophore-grafting on their recognition properties was investigated.

Keywords: AMD070; CXCR4; Fluorescence.

MeSH terms

  • Benzylamines / chemical synthesis
  • Benzylamines / chemistry
  • Benzylamines / pharmacology
  • Cell Line, Tumor
  • Humans
  • Molecular Structure
  • Receptors, CXCR4* / antagonists & inhibitors
  • Receptors, CXCR4* / metabolism
  • Structure-Activity Relationship

Substances

  • Benzylamines
  • CXCR4 protein, human
  • Receptors, CXCR4
  • mavorixafor