Novel 4-Amino-Quinazoline moieties ligated Platinum(IV) prodrugs overcome cisplatin resistance in EGFRWT human lung cancer

Li, Rui; Zhao, Weiheng; Jin, Chen; Xiong, Huihua

doi:10.1016/j.bioorg.2023.106499

Cited by 2 publications

(2 citation statements)

References 39 publications

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“…24). 89 The introduced axial ligand conferred them with enhanced antiproliferative activities with respect to a Pt( iv ) analog without the EGFR inhibitor motif and comparable activities to cisplatin and oxaliplatin in several cell lines (A549, A431, H1299, H1975). Conjugate 50 was selected as lead compound; its cell uptake in both sensitive and cisplatin-resistant A549 cells was shown to be 3 to 4 times larger than that of oxaliplatin or cisplatin.…”

Section: Oxaliplatin-based Pt(iv) Prodrugsmentioning

confidence: 99%

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

Lopez-Sanchez,

Bertrand

2024

Inorg. Chem. Front.

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Section: Oxaliplatin-based Pt(iv) Prodrugsmentioning

confidence: 99%

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

Lopez-Sanchez,

Bertrand

2024

Inorg. Chem. Front.

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“…15 Thus, this manuscript describes the general design, synthesis, characterization, and biological activity of multitargeting Pt(IV) prodrugs that combine cisplatin and dasatinib. While there are reports on Pt(IV) prodrugs that were conjugated to partial scaffolds of imatinib and nilotinib by rigid linkers 16,17 and to 4-aminoquinazoline derivatives, 18 they do not release approved tyrosine kinase inhibitors (TKIs). To our knowledge, this is the first report on a Pt(IV) prodrug conjugated to an FDAapproved TKI.…”

Section: ■ Introductionmentioning

confidence: 99%

Multiaction Pt(IV) Prodrugs Releasing Cisplatin and Dasatinib Are Potent Anticancer and Anti-Invasive Agents Displaying Synergism between the Two Drugs

Markova,

Maji,

Kostrhunova

et al. 2024

J. Med. Chem.

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Herein, we describe the general design, synthesis, characterization, and biological activity of new multitargeting Pt(IV) prodrugs that combine antitumor cisplatin and dasatinib, a potent inhibitor of Src kinase. These prodrugs exhibit impressive antiproliferative and anti-invasive activities in tumor cell lines in both two-dimensional (2D) monolayers of cell cultures and three-dimensional (3D) spheroids. We show that the cisplatin moiety and dasatinib in the investigated Pt(IV) complexes are both involved in the mechanism of action in MCF7 breast cancer cells and act synergistically. Thus, combining dasatinib and cisplatin into one molecule, compared to using individual components in a mix, may bring several advantages, such as significantly higher activity in cancer cell lines and higher selectivity for tumor cells. Most importantly, Pt(IV)-dasatinib complexes hold significant promise for potential anticancer therapies by targeting epithelial–mesenchymal transition, thus preventing the spread and metastasis of tumors, a value unachievable by a simple combination of both individual components.

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Novel 4-Amino-Quinazoline moieties ligated Platinum(IV) prodrugs overcome cisplatin resistance in EGFRWT human lung cancer

Cited by 2 publications

References 39 publications

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

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

Multiaction Pt(IV) Prodrugs Releasing Cisplatin and Dasatinib Are Potent Anticancer and Anti-Invasive Agents Displaying Synergism between the Two Drugs

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