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  • Title: Squaraines bearing halogenated moieties as anticancer photosensitizers: Synthesis, characterization and biological evaluation.
    Author: Serpe L, Ellena S, Barbero N, Foglietta F, Prandini F, Gallo MP, Levi R, Barolo C, Canaparo R, Visentin S.
    Journal: Eur J Med Chem; 2016 May 04; 113():187-97. PubMed ID: 26942626.
    Abstract:
    We report the synthesis and characterization of a series of symmetrical indolenine-based squaraine dyes along with the evaluation of their singlet oxygen generation efficiency. The photodynamic activity of these new photosensitizers has been evaluated on a human tumor fibrosarcoma (HT-1080) cell line. The cytotoxicity increased over time and is induced by the photoactivation of bromo (Br-C4) and iodio (I-C4) long carbon chain squaraine dyes and the consequent increase in reactive oxygen species (ROS) production (p < 0.001), which leads to necrosis 6 h after treatment. Induction of cytochrome c release, DNA damage and up-regulation of GPX1, NQO1 and SOD2 mRNA gene expression after PDT were investigated.
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