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JOURNAL ARTICLE
RESEARCH SUPPORT, NON-U.S. GOV'T
The evaluations of 99m Tc cyclopentadienyl tricarbonyl triphenyl phosphonium cation for multidrug resistance.
Bioorganic & Medicinal Chemistry Letters 2017 August 2
A triphenylphosphonium cation, [99m Tc]Technetium cyclopentadienyltricarbonyl-6-hexanoyl-triphenylphosphonium cation ([99m Tc]3) was prepared to target multidrug resistance (MDR). The radiotracer was evaluated in the MDR-negative MCF-7 and MDR-positive MCF-7/ADR cell lines in vitro, as well as animal models in vivo. [99m Tc]3 was proofed to be a substrate of P-glycoprotein and multidrug resistant protein 1, and showed a higher accumulation in the MDR-negative MCF-7 cells compared to99m Tc-sestamibi in vitro. The MCF-7 tumor-to-MCF-7/ADR tumor ratio of [99m Tc]3 was ∼3 at 1hp.i. in the biodistribution study. These results demonstrated the capability of the radiotracer to detect multidrug resistance in tumor cells.
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