Targeting of G‐quadruplex DNA with <sup>99m</sup>Tc(I)/Re(I) Tricarbonyl Complexes Carrying Pyridostatin Derivatives
作者:Elisa Palma、Cigdem Içhedef、Célia Fernandes、Ana Belchior、Paula Raposinho、Lurdes Gano、André Miranda、David Moreira、Pedro Lourenço、Carla Cruz、Ana Salomé Pires、Maria Filomena Botelho、António Paulo
DOI:10.1002/chem.202400285
日期:2024.4.16
New (Radio)metalated G4 binders: Re(I) and 99mTc(I) complexes carrying pyridostatin derivatives for the targeting of G-quadruplex structures. The Re complex can bind to G4 DNA and RNA with selectivity over double-stranded DNA, exhibiting cytotoxic activity in MCF-7 human breast cancer and PC3 human prostate cancer cell lines. The 99mTc congener is stable in vivo with a fast blood clearance in normal
新型(放射性)金属化 G4 结合剂:带有吡啶他汀衍生物的 Re(I) 和99m Tc(I) 配合物,用于靶向 G-四链体结构。 Re 复合物可以比双链 DNA 选择性地结合 G4 DNA 和 RNA,在 MCF-7 人乳腺癌和 PC3 人前列腺癌细胞系中表现出细胞毒活性。 99m Tc 同源物在体内稳定,在正常小鼠中具有快速的血液清除率。