2. Academic Validation
  3. Synthesis and evaluation of novel meso-substitutedphenyl dithieno[3,2-b]thiophene-fused BODIPY derivatives as efficient photosensitizers for photodynamic therapy

Synthesis and evaluation of novel meso-substitutedphenyl dithieno[3,2-b]thiophene-fused BODIPY derivatives as efficient photosensitizers for photodynamic therapy

  • Eur J Med Chem. 2023 Nov 30:264:116012. doi: 10.1016/j.ejmech.2023.116012.
Ning Cao 1,  Ying Jiang 1,  Zhi-Bing Song 1,  Danye Chen 2,  Dan Wu 3,  Zhi-Long Chen 4,  Yi-Jia Yan 5
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Science & Technology, Donghua University, Shanghai, 201620, China.
  • 2 Department of Chemistry, Imperial College of London, London, SW72AZ, UK.
  • 3 Department of Chemistry, Royal College of Surgeons, 123 St Stephen's Green, Dublin, 2, Ireland.
  • 4 Department of Pharmaceutical Science & Technology, Donghua University, Shanghai, 201620, China; Department of Pharmacy, Huadong Hospital, Fudan University, Shanghai, 200040, China. Electronic address: zlchen1967@qq.com.
  • 5 Department of Pharmacy, Huadong Hospital, Fudan University, Shanghai, 200040, China; Shanghai Xianhui Pharmaceutical Co., Ltd., Shanghai, 201620, China. Electronic address: y_yan11@sina.com.
PMID: 38056302 DOI: 10.1016/j.ejmech.2023.116012
Abstract

The discovery of new photosensitizer drugs with long wavelength Uv-vis absorption, high efficiency and low side-effects is still a challenge in photodynamic therapy. Here a series of novel meso-substitutedphenyl thieno[3,2-b]thiophene-fused BODIPY derivatives were designed, synthesized and characterized. All these compounds have strong absorption at 640-680 nm and obvious fluorescence emission at 650-760 nm. They exhibited high singlet oxygen generation ability and significant photodynamic efficiency against Eca-109 Cancer cells. Compounds II4, II6, II9, II10 and II13 could generate intracellular ROS and induce cell Apoptosis after laser irradiation, which displayed superior photodynamic efficiency against Eca-109 cells than Temoporfin in vitro and in vivo. Among them, compound II4 specifically exhibited excellent anti-tumor efficacy, and could be selected as a new drug candidate for PDT.

Keywords

Anti-Tumor; Photodynamic therapy; Photosensitizer; TT-BODIPY.

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