School of Chemistry, SFI Tetrapyrrole Laboratory, Trinity Biomedical Sciences Institute, Trinity College Dublin, The University of Dublin, 152-160 Pearse Street, Dublin 2, Ireland.
Department of Chemistry, University of Hull, Cottingham Road, Kingston-upon-Hull, HU6 7RX, UK.
Photochem Photobiol Sci. 2019 Feb 13;18(2):495-504. doi: 10.1039/c8pp00402a.
The facile synthesis and in vitro activity of a library of heavy atom-free BODIPY-anthracene, -pyrene dyads (BAD-13-BPyrD-19) and a control (BODIPY 20) are reported. We demonstrate that singlet oxygen produced from dyad triplet states formed from charge-separated states is sufficient to induce cytotoxicity in human breast cancer cells (MDA-MB-468) at micromolar concentrations. The compounds in this series are promising candidates for photodynamic therapy, especially BAD-17 which displays significant photocytotoxicity (15% cell viability) at a concentration of 5 × 10-7 M, with minimal toxicity (89% cell viability) in the absence of light.
报告了一系列无重原子的 BODIPY-蒽、-芘二聚体（BAD-13-BPyrD-19）和对照物（BODIPY 20）的简便合成和体外活性。我们证明，从电荷分离态形成的二聚体三重态产生的单线态氧足以在微摩尔浓度下诱导人乳腺癌细胞（MDA-MB-468）的细胞毒性。该系列化合物是光动力疗法的有前途的候选物，特别是 BAD-17 在 5×10-7 M 的浓度下显示出显著的光细胞毒性（15%细胞活力），在没有光的情况下毒性最小（89%细胞活力）。
