Pt(<scp>iv</scp>) anticancer prodrugs bearing an oxaliplatin scaffold: what do we know about their bioactivity?

Lopez-Sanchez, Alvaro; Bertrand, Helene C.

doi:10.1039/d3qi02602g

Cited by 3 publications

(1 citation statement)

References 154 publications

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“…Platinum(IV) anticancer agents represent a promising and evolving class of compounds that have garnered attention for their distinct properties and potential advantages over traditional platinum(II) drugs [ 8 ]. In fact, some Pt(IV) complexes exhibit enhanced stability, reduced side effects and the ability to release active platinum(II) species preferentially within cancer cells.…”

Section: Introductionmentioning

confidence: 99%

Platinum(0)-η2-1,2-(E)ditosylethene Complexes Bearing Phosphine, Isocyanide and N-Heterocyclic Carbene Ligands: Synthesis and Cytotoxicity towards Ovarian and Breast Cancer Cells

Compagno,

Piccolo,

Bortolamiol

et al. 2024

Molecules

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A wide range of platinum(0)-η2-(E)-1,2-ditosylethene complexes bearing isocyanide, phosphine and N-heterocyclic carbene ancillary ligands have been prepared with high yields and selectivity. All the novel products underwent thorough characterization using spectroscopic techniques, including NMR and FT-IR analyses. Additionally, for some compounds, the solid-state structures were elucidated through X-ray diffractometry. The synthesized complexes were successively evaluated for their potential as anticancer agents against two ovarian cancer cell lines (A2780 and A2780cis) and one breast cancer cell line (MDA-MB-231). The majority of the compounds displayed promising cytotoxicity within the micromolar range against A2780 and MDA-MB-231 cells, with IC50 values comparable to or even surpassing those of cisplatin. However, only a subset of compounds was cytotoxic against cisplatin-resistant cancer cells (A2780cis). Furthermore, the assessment of antiproliferative activity on MRC-5 normal cells revealed certain compounds to exhibit in vitro selectivity. Notably, complexes 3d, 6a and 6b showed low cytotoxicity towards normal cells (IC50 > 100 µM) while concurrently displaying potent cytotoxicity against cancer cells.

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Section: Introductionmentioning

confidence: 99%

Platinum(0)-η2-1,2-(E)ditosylethene Complexes Bearing Phosphine, Isocyanide and N-Heterocyclic Carbene Ligands: Synthesis and Cytotoxicity towards Ovarian and Breast Cancer Cells

Compagno,

Piccolo,

Bortolamiol

et al. 2024

Molecules

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Palladium(II)-Indenyl Complexes Bearing N-Heterocyclic Carbene (NHC) Ligands as Potent and Selective Metallodrugs toward High-Grade Serous Ovarian Cancer Models

Bortolamiol,

Mauceri,

Piccolo

et al. 2024

J. Med. Chem.

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In this study, we synthesized novel Pd(II)-indenyl complexes using various N-heterocyclic carbene (NHC) ligands, including chelating NHC-picolyl, NHC-thioether, and diNHC ligands, and two monodentate NHCs. Transmetalation reactions between a Pd(II)-indenyl precursor and silver-NHC complexes were generally employed, except for chelating diNHC derivatives, which required direct reaction with bisimidazolium salts and potassium carbonate. Characterization included NMR, HRMS analysis, and single-crystal X-ray diffraction. In vitro on five ovarian cancer cell lines showed notable cytotoxicity, with IC50 values in the micro- and submicromolar range. Some compounds exhibited intriguing selectivity for cancer cells due to higher tumor cell uptake. Mechanistic studies revealed that monodentate NHCs induced mitochondrial damage while chelating ligands caused DNA damage. One chelating NHC-picolyl ligand showed promising cytotoxicity and selectivity in high-grade serous ovarian cancer models, supporting its consideration for preclinical study.

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Structurally diverse zinc(ii) complexes containing tripodal tetradentate phenoxido-amines with promising antiproliferative effects

Massoud,

Mautner,

Louka

et al. 2024

Dalton Trans.

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Pt(iv) anticancer prodrugs bearing an oxaliplatin scaffold: what do we know about their bioactivity?

Abstract: Cancer remains a significant global health challenge, necessitating continuous advancements in therapeutic strategies. Chemotherapeutic agents have long been pivotal in cancer treatment, with Platinum(Pt)-based drugs holding a prominent place. Oxaliplatin,...

Cited by 3 publications

References 154 publications

Platinum(0)-η2-1,2-(E)ditosylethene Complexes Bearing Phosphine, Isocyanide and N-Heterocyclic Carbene Ligands: Synthesis and Cytotoxicity towards Ovarian and Breast Cancer Cells

Platinum(0)-η2-1,2-(E)ditosylethene Complexes Bearing Phosphine, Isocyanide and N-Heterocyclic Carbene Ligands: Synthesis and Cytotoxicity towards Ovarian and Breast Cancer Cells

Palladium(II)-Indenyl Complexes Bearing N-Heterocyclic Carbene (NHC) Ligands as Potent and Selective Metallodrugs toward High-Grade Serous Ovarian Cancer Models

Structurally diverse zinc(ii) complexes containing tripodal tetradentate phenoxido-amines with promising antiproliferative effects

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