Lameijer Lucien N, Brevé Tobias G, van Rixel Vincent H S, Askes Sven H C, Siegler M A, Bonnet Sylvestre
Leiden Institute of Chemistry, Leiden University, Gorlaeus Laboratories, P.O. Box 9502, 2300 RA, Leiden, The Netherlands.
Departement of Chemistry, Johns Hopkins University, Baltimore, Maryland, 21218, USA.
Chemistry. 2018 Feb 21;24(11):2709-2717. doi: 10.1002/chem.201705388. Epub 2018 Jan 30.
Ruthenium polypyridyl complexes have received widespread attention as potential chemotherapeutics in photodynamic therapy (PDT) and in photochemotherapy (PACT). Here, we investigate a series of sixteen ruthenium polypyridyl complexes with general formula [Ru(tpy)(N-N)(L)] (tpy=2,2':6',2''-terpyridine, N-N=bpy (2,2'-bipyridine), phen (1,10-phenanthroline), dpq (pyrazino[2,3-f][1,10]phenanthroline), dppz (dipyrido[3,2-a:2',3'-c]phenazine, dppn (benzo[i]dipyrido[3,2-a:2',3'-c]phenazine), pmip (2-(4-methylphenyl)-1H-imidazo[4,5-f][1,10]phenanthroline), pymi ((E)-N-phenyl-1-(pyridin-2-yl)methanimine), or azpy (2-(phenylazo)pyridine), L=Cl or 2-(2-(2-(methylthio)ethoxy)ethoxy)ethyl-β-d-glucopyranoside) and their potential for either PDT or PACT. We demonstrate that although increased lipophilicity is generally related to increased uptake of these complexes, it does not necessarily lead to increased (photo)cytotoxicity. However, the non-toxic complexes are excellent candidates as PACT carriers.
钌多吡啶配合物作为光动力疗法（PDT）和光化学疗法（PACT）中的潜在化疗药物受到了广泛关注。在此，我们研究了一系列十六种通式为[Ru(tpy)(N-N)(L)]的钌多吡啶配合物（tpy = 2,2':6',2''-三联吡啶，N-N = bpy（2,2'-联吡啶）、phen（1,10-菲咯啉）、dpq（吡嗪并[2,3-f][1,10]菲咯啉）、dppz（二吡啶并[3,2-a:2',3'-c]吩嗪）、dppn（苯并[i]二吡啶并[3,2-a:2',3'-c]吩嗪）、pmip（2-(4-甲基苯基)-1H-咪唑并[4,5-f][1,10]菲咯啉）、pymi（(E)-N-苯基-1-(吡啶-2-基)甲亚胺）或azpy（2-(苯基偶氮)吡啶），L = Cl或2-(2-(2-(甲硫基)乙氧基)乙氧基)乙基-β-D-吡喃葡萄糖苷）及其在PDT或PACT中的潜力。我们证明，尽管亲脂性增加通常与这些配合物的摄取增加有关，但这不一定会导致（光）细胞毒性增加。然而，无毒的配合物是作为PACT载体的极佳候选物。
