Platinum(II) ring-fused chlorins as efficient theranostic agents: Dyes for tumor-imaging and photodynamic therapy of cancer

• Autor(es): Laranjo, Mafalda ; Aguiar, Márcia Campos ; Pereira, Nelson A. M. ; Brites, Gonçalo ; Nascimento, Bruno F. O. ; Brito, Ana F. ; Casalta-Lopes, João ; Gonçalves, Ana Cristina ; Sarmento-Ribeiro, Ana Bela ; Piñeiro Gomez, Marta ; Botelho, Maria Filomena ; Melo, Teresa M. V. D. Pinho e
• Data: 2020
• Identificador Persistente: https://hdl.handle.net/10316/93139
• Origem: Estudo Geral - Universidade de Coimbra
• Assunto(s): Animal models; Bladder carcinoma; Luminescence imaging; Melanoma; Oesophageal carcinoma; Optical imaging; Photodynamic therapy; Photosensitizers; Pt(II) chlorins; Theranostics; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Coordination Complexes; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Esophageal Neoplasms; Fluorescent Dyes; Humans; Melanoma; Molecular Structure; Platinum; Porphyrins; Structure-Activity Relationship; Urinary Bladder Neoplasms; Optical Imaging; Photochemotherapy
• Tipo de Documento: Artigo científico
• Idioma: Inglês

Descrição

The discovery of Pt-chlorin-type theranostic agents is described. Luminescent Pt(II) 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-fused chlorins, with different degrees of hydrophilicity, have been synthesized and their in vitro photocytotoxicity against human melanoma, oesophageal and bladder carcinomas was studied. A di(hydroxymethyl)-substituted chlorin was identified as a privileged molecule to explore imaging-guided photodynamic therapy. In addition to the high activity as PDT agent and absence of cytotoxicity per se, this molecule showed the ideal photophysical and photochemical properties. In vivo studies using a A375 melanoma mouse model, proved the extraordinary properties of this chlorin as a luminescent probe and the ability to impair tumor growth, making image guided treatment and follow up a possibility.