Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 58, Issue 40, Pages 14334-14340Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201907856
Keywords
antitumor agents; bioinorganic chemistry; photodynamic therapy; photosensitizers; zinc
Categories
Funding
- ERC [GA 681679]
- program Investissements d'Avenir [ANR-10-IDEX-0001-02 PSL]
- National Science Foundation of China [21525105, 21778079]
- 973 Program [2015CB856301]
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The use of photodynamic therapy (PDT) to treat cancer has received increasing attention over the last years. However, the clinically used photosensitisers (PSs) have some limitations that include poor aqueous solubility, hepatotoxicity, photobleaching, aggregation, and slow clearance from the body, so the design of new classes of PSs is of great interest. We present the use of bis(dipyrrinato)zinc(II) complexes with exceptionally long lifetimes as efficient PDT PSs. Based on the heavy-atom effect, intersystem crossing of these complexes changes the excited state from singlet to a triplet state, thereby enabling singlet oxygen generation. To overcome the limitation of quenching effects in water and improve water solubility, the lead compound 3 was encapsulated in a polymer matrix. It showed impressive phototoxicity upon irradiation at 500 nm in various monolayer cancer cells as well as 3D multicellular tumour spheroids, without observed dark toxicity.
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