ArticleActa pharmaceutica Sinica. B2026
Dual-modal tumor-selective benzofuran tracer integrating real-time imaging and anticancer effects.
Article in Acta pharmaceutica Sinica. B, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Microtubule-targeting agents remain a cornerstone of cancer therapy; however, few compounds can simultaneously visualize intratumoral distribution and correlate pharmacodynamics with therapeutic response. Here, we describe BF-04, a Benzofuran-derived microtubule destabilizer that circumvents multidrug resistance and integrates anticancer efficacy with dual-modality imaging. Chemical conjugation with the Cyanine 5 fluorescent dye (Cy5) and Zirconium-89 (89Zr) provided high-contrast, real-time fluorescence and Positron emission tomography (PET) signals without the need for antibody or nanoparticle carriers, enabling direct monitoring of drug distribution and retention in tumors. Importantly, BF-04 exhibited tumor-selective accumulation independent of labeling, confirming a scaffold-driven targeting mechanism with strong translational potential for image-guided therapy. Mechanistically, BF-04 induced microtubule depolymerization, mitotic arrest, and apoptosis across multiple cancer cell lines and patient-derived organoids (PDOs).
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