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<p>Aggregation-Induced Emission (AIE) fluorophores play more and more essential roles in imaging-based diagnosis and photoinduced therapy due to their unique optical properties. However, most AIE units, such as tetraphenylethene, hexaphenylsilole and distyrylanthracene, emit in short wavelength region, normally blue to green. Thus designing and synthesizing near-infrared (NIR) AIE emitters remains significantly challenging, especially for those with emission wavelengths &gt; 800&#xa0;nm. Fortunately, we successfully designed and synthesized a series of AIE-active NIR fluorophores (<b>TTN-1</b> to <b>TTN-4</b>) based on a naphthothiadiazole (NT) core in this study. Featuring a donor-π-acceptor-π-donor (D-π-A-π-D) backbone, these dyes enjoy NIR-I emission up to 823&#xa0;nm owning to the extended π-conjugation and enhanced intramolecular electron push-pull effect. Their multi-rotor architectures and highly twisted molecular configurations also endow them with typical aggregation-induced emission (AIE) characteristic. Meanwhile all of them enjoy the capability of efficient reactive oxygen species (ROS) generation upon light irradiation. In further biological evaluations, antibody-conjugated <b>TTN-4</b> nanoparticles enabled precise squamous cell carcinoma (SCC) cells targeting and high-contrast intraoperative tumor imaging, rendering them as promising theranostic agents for hand SCC treatment.</p>

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Development of AIE-active Near-infrared Emitters Based on Naphthothiadiazoles and Their Theronostic Applications in Squamous Cell Carcinoma

  • 期刊论文

  • 发表日期：

    2026年4月24日

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  • Huabin He,
  • Man Zhou

摘要

Aggregation-Induced Emission (AIE) fluorophores play more and more essential roles in imaging-based diagnosis and photoinduced therapy due to their unique optical properties. However, most AIE units, such as tetraphenylethene, hexaphenylsilole and distyrylanthracene, emit in short wavelength region, normally blue to green. Thus designing and synthesizing near-infrared (NIR) AIE emitters remains significantly challenging, especially for those with emission wavelengths > 800 nm. Fortunately, we successfully designed and synthesized a series of AIE-active NIR fluorophores (TTN-1 to TTN-4) based on a naphthothiadiazole (NT) core in this study. Featuring a donor-π-acceptor-π-donor (D-π-A-π-D) backbone, these dyes enjoy NIR-I emission up to 823 nm owning to the extended π-conjugation and enhanced intramolecular electron push-pull effect. Their multi-rotor architectures and highly twisted molecular configurations also endow them with typical aggregation-induced emission (AIE) characteristic. Meanwhile all of them enjoy the capability of efficient reactive oxygen species (ROS) generation upon light irradiation. In further biological evaluations, antibody-conjugated TTN-4 nanoparticles enabled precise squamous cell carcinoma (SCC) cells targeting and high-contrast intraoperative tumor imaging, rendering them as promising theranostic agents for hand SCC treatment.