Enhancement of cytotoxicity by combining pyrenyl-dendrimers and arene ruthenium metallacages.
Three generations of pyrenyl bis-MPA dendrimers with two different end-groups, acetonide (pyr(Gn)) or alcohol (pyr(Gn-OH)) (n = 1-3), were synthesized, and the pyrenyl group of the dendritic molecules was encapsulated in the arene ruthenium metallacages, [Ru(6)(p-cymene)(6)(OO∩OO)(3)(tpt)(2)](6+) (OO∩OO = 5,8-dioxydo-1,4-naphtaquinonato (donq) [1](6+) and 6,11-dioxydo-5,12-naphtacenedionato (dotq) [2](6+); tpt =2,4,6-tri(pyridin-4-yl)-1,3,5-triazine). The host-guest properties of [guest⊂1](6+) and [guest⊂2](6+) were studied in solution by NMR and UV-vis spectroscopic methods, thus allowing the determination of the affinity constants. Moreover, the cytotoxicity of these water-soluble host-guest systems and the pyrenyl-dendrimers was evaluated on human ovarian cancer cells.
Institut de Chimie, Université de Neuchâtel, Avenue de Bellevaux 51, CH-2000 Neuchâtel, Switzerland.
Anaïs
A
Pitto-Barry
Olivier
O
Zava
Paul J
PJ
Dyson
Robert
R
Deschenaux
Bruno
B
Therrien
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D050091:Dendrimers / Q000138:chemical synthesis / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011721:Pyrenes / Q000737:chemistry*; D012428:Ruthenium / Q000737:chemistry*; D012995:Solubility; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D050091:Dendrimers; D009942:Organometallic Compounds; D011721:Pyrenes; D012428:Ruthenium