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Flavin-Conjugated Pt(IV) Anticancer Agents by Juan Sánchez-Camacho; Sonia Infante-Tadeo; Ana C. Carrasco; Stefano Scoditti; Álvaro Martínez; Fabienne Barroso-Bujans; Emilia Sicilia; Ana M. Pizarro; Luca Salassa is a Chemistry article available to read on EtoBox.
What is Flavin-Conjugated Pt(IV) Anticancer Agents about?
In situ activation of Pt(IV) to Pt(II) species is a promising strategy to control the anticancer activity and overcome the off-target toxicity linked to classic platinum chemotherapeutic agents. Herein, we present the design and synthesis of two new asymmetric Pt(IV) derivatives of cisplatin and oxaliplatin (1•TARF and 2•TARF, respectively) bearing a covalently bonded 2′,3′,4′,5′tetraacetylriboflavin moiety (TARF). 1 H and 195 Pt NMR spectroscopy shows that 1•TARF and 2•TARF can be effectively activated into toxic Pt(II) species, when incubated with nicotinamide adenine dinucleotide, sodium ascorbate, and glutathione in the dark and under light irradiation. Density functional theory studies of the dark Pt(IV)-to-Pt(II) conversion of 2•TARF indicate that the process involves first hydride transfer from the donor to the flavin moiety of the complex, followed by electron transfer to the Pt(IV) center. When administered to MDA-MB-231 breast cancer cells preincubated with nontoxic amounts of ascorbate, 2•TARF displays enhanced toxicity (between 1 and 2 orders of magnitude), suggesting that the generation of oxaliplatin can selectively be triggered by redox activation. Such an effect is
Who reads Flavin-Conjugated Pt(IV) Anticancer Agents?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Juan Sánchez-Camacho; Sonia Infante-Tadeo; Ana C. Carrasco; Stefano Scoditti; Álvaro Martínez; Fabienne Barroso-Bujans; Emilia Sicilia; Ana M. Pizarro; Luca Salassa
- Publisher
- American Chemical Society (ACS)
- Published
- 2023
- Language
- EN
- Field
- Chemistry (Physical Sciences)