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.
- 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: [email protected].
- 5. Department of Pharmacy, Huadong Hospital, Fudan University, Shanghai, 200040, China; Shanghai Xianhui Pharmaceutical Co., Ltd., Shanghai, 201620, China. Electronic address: [email protected].
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.
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