Abstract
The role of autophagy in cancer is often complex, ranging from tumor‐promoting to ‐suppressing effects. In this study, two novel hybrid molecules were designed, containing a ruthenacarborane fragment conjugated with a known modulator of autophagy, namely a quinoline derivative. The complex closo‐[3‐(η 6‐p‐cymene)‐1‐(quinolin‐8‐yl‐acetate)‐3,1,2‐RuC2B9H10] (4) showed a dual mode of action against the LN229 (human glioblastoma) cell line, where it inhibited tumor‐promoting autophagy, and strongly inhibited cell proliferation, de facto blocking cellular division. These results, together with the tendency to spontaneously form nanoparticles in aqueous solution, make complex 4 a very promising drug candidate for further studies in vivo, for the treatment of autophagy‐prone glioblastomas.
Highlights
Introduction particles to ca100 nm,[9] which falls within the optimal size range for application of nanoparticle-based drug delivery technologies, in terms of cellular uptake and clearance pathways.[11]
This spontaneous property of the metallacarborane fragment is well-suited for designing novel chemotherapeutic agents to target those types of tumor, where nanosized chemotherapeutics might provide superior efficacy compared to non-nano-sized drug formulations, due to the characteristics of the tumor itself, as proposed recently, for example, for brain tumors of the glioblastoma type (GBM).[12]
Quinoline derivatives possess a plethora of biological activities,[13a,b] which have prompted the development of numerous drugs, ranging from antiparasitic (e. g. chloroquine and its ferrocene analogue ferroquine), to antiviral (e. g. saquinavir), antibacterial (e. g. ciprofloxacin), antiinflammatory (e. g. quinoline alkaloids), antioxidant
Summary
100 nm,[9] which falls within the optimal size range for application of nanoparticle-based drug delivery technologies, in terms of cellular uptake and clearance pathways.[11] this spontaneous property of the metallacarborane fragment is well-suited for designing novel chemotherapeutic agents to target those types of tumor, where nanosized chemotherapeutics might provide superior efficacy compared to non-nano-sized drug formulations, due to the characteristics of the tumor itself, as proposed recently, for example, for brain tumors of the glioblastoma type (GBM).[12]. Quinoline derivatives possess a plethora of biological activities,[13a,b] which have prompted the development of numerous drugs, ranging from antiparasitic (e. g. chloroquine and its ferrocene analogue ferroquine), to antiviral (e. g. saquinavir), antibacterial (e. g. ciprofloxacin), antiinflammatory (e. g. quinoline alkaloids), antioxidant
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