University of Coimbra, Institute of Biophysics and Institute for Clinical and Biomedical Research (iCBR), Area of Environment Genetics and Oncobiology (CIMAGO), Faculty of Medicine, Portugal; University of Coimbra, Center for Innovative Biomedicine and Biotechnology (CIBB), Portugal; University of Coimbra, Clinical and Academic Centre of Coimbra, Portugal.
University of Coimbra, Institute of Biophysics and Institute for Clinical and Biomedical Research (iCBR), Area of Environment Genetics and Oncobiology (CIMAGO), Faculty of Medicine, Portugal; University of Coimbra, Coimbra Chemistry Centre and Department of Chemistry, 3004-535, Coimbra, Portugal.
Eur J Med Chem. 2020 Aug 15;200:112468. doi: 10.1016/j.ejmech.2020.112468. Epub 2020 May 16.
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.
铂-卟啉型治疗药物的发现。本文描述了一系列具有不同亲水程度的发光 Pt(II) 4,5,6,7-四氢吡唑并[1,5-a]吡啶稠合卟啉的合成，并研究了它们对人黑色素瘤、食管和膀胱癌的体外光细胞毒性。一种二（羟甲基）取代的卟啉被鉴定为一种探索成像引导光动力治疗的优势分子。除了作为 PDT 药物的高活性和本身无细胞毒性外，该分子还表现出理想的光物理和光化学性质。在 A375 黑色素瘤小鼠模型的体内研究中，证明了这种卟啉作为发光探针的非凡特性及其抑制肿瘤生长的能力，使图像引导治疗和随访成为可能。
