A Simple Route toward Next-Generation Thiobase-Based Photosensitizers for Cancer Theranostics

Van Nghia Nguyen, Seonye Heo, Chang Woo Koh, Jeongsun Ha, Gyoungmi Kim, Sungnam Park, Juyoung Yoon

Research output: Contribution to journalArticlepeer-review

17 Scopus citations


Sulfur-substituted biocompatible carbonyl fluorophores have been recognized as effective heavy-atom-free photosensitizers (PSs) for cancer therapy due to their remarkable phototherapeutic properties. However, guidelines on their molecular design are still a substantial challenge. Most of the existing thiocarbonyl-based PSs are nonemissive in both the solution and restricted states, which hinders their further biomedical applications. Herein, we report the interesting finding that sulfur-substituted coumarins exhibit an uncommon phenomenon, aggregation-induced emission. More intriguingly, we also found that the introduction of a strong electron-accepting trifluoromethyl group is crucial to facilitate the mitochondrial-targeting ability of neutral coumarin fluorophores. The resulting CMS-2 PS displayed selective imaging of mitochondria and exhibited much higher photodynamic therapy efficiency toward cancer cells than that of the commercial PS erythrosine B. This work provides deep insight into the molecular design of heavy-atom-free thiobase-based PSs and simultaneously offers a great opportunity to develop novel mitochondrial-targeting fluorescent indicators with neutral bioinspired platforms.

Original languageEnglish
Pages (from-to)3462-3467
Number of pages6
JournalACS Sensors
Issue number9
StatePublished - 24 Sep 2021

Bibliographical note

Funding Information:
This study was supported by grants from the National Research Foundation of Korea (NRF) funded by the Korean government (MSIP) (no. 2012R1A3A2048814 for J.Y. and no. 2019R1A6A1A11044070 for S.P.). The high-resolution mass spectrometry analysis was performed on a Synapt G2-HDMS mass spectrometer (Waters, Manchester, U.K.) operating on MassLynx 4.1 software at KBSI (Korea Basic Science Institute, Ochang, Center of Research Equipment).

Publisher Copyright:
© 2021 American Chemical Society


  • aggregation-induced emission
  • fluorescent probes
  • mitochondrial imaging
  • photodynamic therapy
  • sulfur-substituted coumarin


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