Squaraines bearing halogenated moieties as anticancer photosensitizers: Synthesis, characterization and biological evaluation

التفاصيل البيبلوغرافية
العنوان: Squaraines bearing halogenated moieties as anticancer photosensitizers: Synthesis, characterization and biological evaluation
المؤلفون: Nadia Barbero, Federica Foglietta, Federica Prandini, Claudia Barolo, Renzo Levi, Roberto Canaparo, Sonja Visentin, Maria Pia Gallo, Silvano Ellena, Loredana Serpe
المصدر: European Journal of Medicinal Chemistry. 113:187-197
بيانات النشر: Elsevier BV, 2016.
سنة النشر: 2016
مصطلحات موضوعية: Models, Molecular, DNA damage, medicine.medical_treatment, Antineoplastic Agents, Photodynamic therapy, 010402 general chemistry, Photochemistry, 01 natural sciences, Photosensitizers, Cancer, Singlet oxygen, Squaraines, Drug Discovery3003 Pharmaceutical Science, Organic Chemistry, Pharmacology, Structure-Activity Relationship, chemistry.chemical_compound, Halogens, Phenols, Drug Discovery, Tumor Cells, Cultured, medicine, Humans, Structure–activity relationship, Cytotoxicity, Cell Proliferation, chemistry.chemical_classification, Reactive oxygen species, Photosensitizing Agents, Cell Death, Dose-Response Relationship, Drug, Molecular Structure, biology, 010405 organic chemistry, Cell growth, Cytochrome c, General Medicine, Combinatorial chemistry, 0104 chemical sciences, chemistry, biology.protein, Drug Screening Assays, Antitumor, Reactive Oxygen Species, Cyclobutanes
الوصف: 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.
تدمد: 0223-5234
DOI: 10.1016/j.ejmech.2016.02.035
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c231fbbb087104dbca25b917391f915
https://doi.org/10.1016/j.ejmech.2016.02.035
Rights: OPEN
رقم الانضمام: edsair.doi.dedup.....1c231fbbb087104dbca25b917391f915
قاعدة البيانات: OpenAIRE
الوصف
تدمد:02235234
DOI:10.1016/j.ejmech.2016.02.035