A benzenesulfonamide derivative as a novel PET radioligand for CXCR4

Yoon Hyeun Oum, Dinesh Shetty, Younghyoun Yoon, Zhongxing Liang, Ronald J. Voll, Mark M. Goodman, Hyunsuk Shim

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5 Scopus citations


CXCR4 is involved in various diseases such as inflammation, tumor growth, and cancer metastasis through the interaction with its natural endogenous ligand, chemokine CXCL12. In an effort to develop imaging probes for CXCR4, we developed a novel small molecule CXCR4-targeted PET agent (compound 5) by combining our established benzenesulfonamide scaffold with a labeling component by virtue of click chemistry. 5 shows nanomolar affinity (IC50 = 6.9 nM) against a known CXCR4 antagonist (TN14003) and inhibits more than 65% chemotaxis at 10 nM in vitro assays. Radiofluorinated compound 5 ([18F]5) demonstrates a competitive cellular uptake against CXCL12 in a dose-dependent manner. Further, microPET images of [18F]5 exhibits preferential accumulation of radioactivity in the lesions of λ-carrageenan-induced paw edema, human head and neck cancer orthotopic xenograft, and metastatic lung cancer of each mouse model.

Original languageBritish English
Article number115240
JournalBioorganic and Medicinal Chemistry
Issue number2
StatePublished - 15 Jan 2020


  • C-X-C chemokine receptor type 4 (CXCR4)
  • CXCL12
  • Head and neck cancer
  • Inflammation
  • Metastasis
  • Molecular imaging probe
  • Positron emission tomography (PET)


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