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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry

IF: 6.8
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An Activatable Heavy-Atom-Free Upconversion Photosensitizer for Targeted Imaging and Treatment of Tumors

Published:5 December 2024 DOI: 10.1021/acs.jmedchem.4c02679
Chao Zhao, Wanlu Sun, Yanyan Zhu, Xiaoyan Huang, Ye Sun, Hai-Yan Wang, Yi Pan, Yi Liu

Abstract

Photodynamic therapy (PDT) is an innovative and promising method for treating tumors that has attracted significant interest but still faces several challenges, such as a lack of selectivity, deep penetration of light, and efficient ROS generation. To address these challenges, we optimized and synthesized a series of photosensitizers and successfully developed a heavy-atom-free near-infrared FUCL photosensitizer NFh-NMe-2. This photosensitizer can generate singlet oxygen (1O2) and induce cellular apoptosis under 808 nm light. For the safe ablation of microtumors in vivo, an activatable FUCL photosensitizer NFh-NTR was developed based on the overexpression of nitroreductase (NTR). NFh-NTR could be activated by NTR, leading to the release of the photosensitizer NFh-NMe-2, restoring the fluorescence signal, and effectively killing tumor cells under 808 nm light irradiation. This work opens new possibilities in the chemical design of an FUCL photosensitizer for cancer treatment.

Substances (6)

Materials
Procduct Name CAS Molecular Formula Supplier Price
Triethylamine 121-44-8 C6H15N 1020 suppliers $9.00-$2730.00
3-Aminophenol 591-27-5 C6H7NO 609 suppliers $10.00-$5190.00
Phosphorus oxitrichloride 10025-87-3 Cl3OP 454 suppliers $22.00-$12720.00
Iodomethane 74-88-4 CH3I 418 suppliers $15.00-$5060.00
Iodoethane 75-03-6 C2H5I 416 suppliers $11.00-$2360.00
2,3,3-Trimethylindolenine 1640-39-7 C11H13N 396 suppliers $6.00-$2109.25

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