Magalhães Álvaro F, Graça Vânia C, Calhelha Ricardo C, Ferreira Isabel C F R, Santos Paulo F
Chemistry Dep. and Chemistry Center - Vila Real (CQ-VR), University of Trás-os-Montes and Alto Douro, 5001-801 Vila Real, Portugal.
Mountain Research Centre (CIMO), Polytechnic Institute of Bragança, Campus de Santa Apolónia, 5300-253 Bragança, Portugal.
Bioorg Med Chem Lett. 2017 Sep 15;27(18):4467-4470. doi: 10.1016/j.bmcl.2017.08.004. Epub 2017 Aug 3.
The synthesis of several aminosquaraine cationic dyes displaying strong absorption within the so-called phototherapeutic window (650-850nm) is described. Their cytotoxicity, under dark and illuminated conditions, was tested against several human tumor cell lines (breast, lung, cervical and hepatocellular carcinomas) and non-tumor porcine liver primary cells. All compounds showed to inhibit the growth of the tumor cells upon irradiation more than in the absence of light, in more or less extension, clearly exhibiting photodynamic activity. The photosensitizing ability against some cell lines, together with the low toxicity for the non-tumor primary PLP2 cells displayed by some of the compounds synthetized, turns them into potential candidates as photosensitizers for PDT.
描述了几种氨基方酸阳离子染料的合成，这些染料在所谓的光疗窗口（650 - 850nm）内显示出强烈吸收。在黑暗和光照条件下，测试了它们对几种人类肿瘤细胞系（乳腺癌、肺癌、宫颈癌和肝癌）以及非肿瘤猪肝脏原代细胞的细胞毒性。所有化合物在光照后均比无光时更能抑制肿瘤细胞生长，或多或少都有明显的光动力活性。某些合成化合物对一些细胞系的光敏化能力以及对非肿瘤原代PLP2细胞的低毒性，使其成为光动力疗法（PDT）光敏剂的潜在候选物。
