Moynihan, Eoin and Bassi, Giada and Ruffini, Andrea and Panseri, Silvia and Montesi, Monica and Velasco-Torrijos, Trinidad and Montagner, Diego (2021) Click Pt(IV)-Carbohydrates Pro-Drugs for Treatment of Osteosarcoma. Frontiers in Chemistry, 9. ISSN 2296-2646

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Abstract

The selectivity vs. cancer cells has always been a major challenge for chemotherapeutic agents and in particular for cisplatin, one of the most important anticancer drugs for the treatment of several types of tumors. One strategy to overtake this challenge is to modify the coordination sphere of the metallic center with specific vectors whose receptors are overexpressed in the tumoral cell membrane, such as monosaccharides. In this paper, we report the synthesis of four novel glyco-modified Pt(IV) pro-drugs, based on cisplatin scaffold, and their biological activity against osteosarcoma (OS), a malignant tumor affecting in particular adolescents and young adults. The sugar moiety and the Pt scaffold are linked exploiting the Copper Azide Alkyne Cycloaddition (CUAAC) reaction, which has become the flagship of click chemistry due to its versatility and mild conditions. Cytotoxicity and drug uptake on three different OS cell lines as well as CSCs (Cancer Stem Cell) are described

Item Type:	Article
Additional Information:	Cite as: Moynihan E, Bassi G, Ruffini A, Panseri S, Montesi M, Velasco-Torrijos T and Montagner D (2021) Click Pt(IV)-Carbohydrates Pro- Drugs for Treatment of Osteosarcoma. Front. Chem. 9:795997. doi: 10.3389/fchem.2021.795997
Keywords:	Pt(IV) prodrugs; cisplatin; sugars; osteosarcoma; cancer stem cells; click chemistry;
Academic Unit:	Faculty of Science and Engineering > Chemistry Faculty of Science and Engineering > Research Institutes > Human Health Institute
Item ID:	17441
Identification Number:	https://doi.org/10.3389/fchem.2021.795997
Depositing User:	Diego Montagner
Date Deposited:	17 Aug 2023 13:15
Journal or Publication Title:	Frontiers in Chemistry
Publisher:	Frontiers in Chemistry
Refereed:	Yes
URI:	Publisher
Use Licence:	This item is available under a Creative Commons Attribution Non Commercial Share Alike Licence (CC BY-NC-SA). Details of this licence are available here

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