NDLI: Is antitumor Pt(IV) complex containing two axial lonidamine ligands a true dual- or multi-action prodrug?

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Is antitumor Pt(IV) complex containing two axial lonidamine ligands a true dual- or multi-action prodrug?

Content Provider	Hyper Articles en Ligne (HAL)
Author	Kasparkova, Jana Kostrhunova, Hana Novohradsky, Vojtech Ma, Lili Zhu, Guangyu Milaeva, Elena, R Shtill, Alexender, A Vinck, Robin Gasser, Gilles Brabec, Viktor Nazarov, Alexey, A
Abstract	Abstract This work studied the mechanism of action of a Pt(IV) complex 2 bearing two axial lonidamine ligands, which are selective inhibitors of aerobic glycolysis. The presence of two lonidamine ligands in 2 compared to the parent Pt(II) complex increased its antiproliferative activity, cellular accumulation, and changed its cell cycle profile and mechanism of cell death. In 3D cell culture, 2 showed exceptional antiproliferative activity with IC50 values as low as 1.6µM in MCF7 cells. The study on the influence of the lonidamine ligands in the Pt complex on glycolysis showed only low potency of ligands to affect metabolic processes in cancer cells, making the investigated complex, not a dual- or multi-action prodrug. However, the Pt(IV) prodrug effectively delivers cytotoxic Pt(II) complex into cancer cells.
Related Links	https://hal.science/hal-03708947/file/Is%20antitumor%20Pt%28IV%29%20complex%20containing%20two%20axial%20lonidamine%20ligands%20a%20true.pdf
ISSN	17565901
e-ISSN	1756591X
DOI	10.1093/mtomcs/mfac048
Journal	Metallomics
Language	English
Publisher	HAL CCSD Royal Society of Chemistry
Publisher Date	2022-06-27
Access Restriction	Open
Subject Keyword	Bioinorganic Chemistry Lonidamine Medicinal Inorganic Chemistry Metals in Medicine Pt(IV) complexes Medicinal Chemistry Chemical Sciences
Content Type	Text
Resource Type	Article
Subject	Chemistry Medicine Metals and Alloys Biomaterials Biochemistry Biophysics Chemical Engineering

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