Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 10, Issue 5, Pages 822-827Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00128
Keywords
Rhenium tricarbonyl; tumor growth inhibition; ovarian cancer; mice xenografts; metallodrug; histopathology
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Funding
- Cornell University
- Office of the Assistant Secretary of Defense for Health Affairs through the Ovarian Cancer Research Program [W81XWH-17-1-0097]
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The rhenium(I) complex fac-[Re(CO)(3)(2,9-dimethyl-1,10-phenanthroline)(OH2)](+) (1) was previously shown to exhibit potent in vitro anticancer activity in a manner distinct from conventional platinum-based drugs (J. Am. Chem. Soc. 2017, 139, 14302-14314). In this study, we report further efforts to explore its aqueous speciation and antitumor activity. The cellular uptake of 1 was measured in A2780 and cisplatin-resistant A2780CP70 ovarian cancer cells by inductively coupled plasma mass spectrometry, revealing similar uptake efficiency in both cell lines. High accumulation in the mitochondria was observed, contradicting prior fluorescence microscopy studies. The luminescence of 1 is highly dependent on pH and coordination environment, making fluorescence microscopy somewhat unreliable for determining compound localization. The in vivo anticancer activity of 1 was evaluated in mice bearing patient-derived ovarian cancer tumor xenografts. These studies conclusively show that 1 is capable of inhibiting tumor growth, providing further credibility for the use of these compounds as anticancer agents.
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