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Title: Platinum(II) ring-fused chlorins as efficient theranostic agents: Dyes for tumor-imaging and photodynamic therapy of cancer
Authors: 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 
Keywords: Animal models; Bladder carcinoma; Luminescence imaging; Melanoma; Oesophageal carcinoma; Optical imaging; Photodynamic therapy; Photosensitizers; Pt(II) chlorins; Theranostics
Issue Date: 15-Aug-2020
Publisher: Elsevier Masson
Project: UIDB/00313/2020 
Serial title, monograph or event: European Journal of Medicinal Chemistry
Volume: 200
Abstract: 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.
ISSN: 02235234
DOI: 10.1016/j.ejmech.2020.112468
Rights: embargoedAccess
Appears in Collections:I&D CQC - Artigos em Revistas Internacionais

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