In photodynamic therapy (PDT), a non-invasive anticancer treatment, visible light is used as a magic bullet selectively destroying cancer cells by a photosensitizer that is non-toxic in the dark. Protoporphyrin IX (PpIX) is a natural photosensitizer synthesized in the cell which is also a chelating agent that if bonded to Fe²⁺ forms heme, a central component of hemoglobin. Therefore, xenobiotic iron chelators can disturb iron homeostasis, increasing the accumulation of PpIX, obstructing the last step of heme biosynthesis, and enhancing PDT efficiency. However, the attempts to use this promising idea have not proved to be hugely successful. Herein, we revisited this issue by analyzing the application of iron chelators highly toxic in the dark which should have higher Fe²⁺affinity than the non-toxic chelators used so far. We have designed and prepared thiosemicarbazones (TSCs) with the highest dark cellular cytotoxicity among TSCs ever reported. We demonstrate that compound 1 and 2 exert powerful PDT enhancement when used in combination with 5-aminolevulinic acid (ALA), a precursor of PpIX.

• Legal notice:
  

  Copyright (c) Pielaszek Research, all rights reserved.
  The above materials, including auxiliary resources, are subject to Publisher's copyright and the Author(s) intellectual rights. Without limiting Author(s) rights under respective Copyright Transfer Agreement, no part of the above documents may be reproduced without the express written permission of Pielaszek Research, the Publisher. Express permission from the Author(s) is required to use the above materials for academic purposes, such as lectures or scientific presentations.
  In every case, proper references including Author(s) name(s) and URL of this webpage: https://science24.com/paper/31186 must be provided.

1. Glutathione depletion and reactive oxygen species generation by thiosemicarbazones in cancer therapy.
2. Synthesis and potential spectrum of biological activities of glycoconjugates derivatives of hydroxy-2-methylquinoline carboxylic acids
3. Studies on anticancer iron chelators
4. Quinoline based antifungals
5. Iron chelators- the novel perspective in cancer treatment
6. The biological activity of sugar derivatives based on quinoline scaffold
7. Structure-Lipophilicity Relationships in Series of Quinoline Derivatives
8. Characterisation of newly obtained Pb(Mn1/3Nb2/3)O3 ceramics by XRD, XPS and dielectric permittivity tests.