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A Pt(IV) Prodrug Combining Chlorambucil and Cisplatin: A Dual-Acting Weapon for Targeting DNA in Cancer Cells
Montagner, Diego; Tolan, Dina; Andriollo, Emma; Gandin, Valentina; Marzano, Cristina
In this study, two DNA-targeting agents, cisplatin and chlorambucil, were combined in a Pt(IV) prodrug, 1, which was thoroughly characterized by means of spectroscopic and spectrometric techniques. Tested towards a panel of various human tumor cell lines, this compound showed superior in vitro antitumor potential than the reference drug cisplatin. In addition, an antitumor potential of 1 was found, which is comparable to that of oxaliplatin in 3D spheroid models of colon cancer cells. Mechanistic studies performed in colon cancer cells confirmed that the conjugation of chlorambucil to Pt(IV) cisplatin-based scaffold tunes the lipophilicity of the prodrug, consequently improving the ability of the compound to accumulate into cancer cells and to target DNA, ultimately leading to apoptotic cancer cell death.
Keyword(s): cisplatin; chlorambucil; Pt(IV) prodrugs; cytotoxicity
Publication Date:
2018
Type: Journal article
Peer-Reviewed: Yes
Institution: Maynooth University
Citation(s): Montagner, Diego and Tolan, Dina and Andriollo, Emma and Gandin, Valentina and Marzano, Cristina (2018) A Pt(IV) Prodrug Combining Chlorambucil and Cisplatin: A Dual-Acting Weapon for Targeting DNA in Cancer Cells. International Journal of Molecular Sciences, 19 (12). p. 3775. ISSN 1422-0067
Publisher(s): MDPI
File Format(s): other
Related Link(s): http://mural.maynoothuniversity.ie/10749/1/DM-Targeting-DNA-2018.pdf
First Indexed: 2020-04-02 06:13:22 Last Updated: 2020-04-02 06:13:22