AuNP Pyrazolo[3,4‑d]pyrimidine Nanosystem in Combination with Radiotherapy against Glioblastoma

Gold-nanoparticle (AuNP)-conjugated drugs represent a promising and innovative antitumor therapeutic approach. In our study, we describe the design, the synthesis, the preparation, and the characterization of AuNPs conjugated with the pyrazolo­[3,4-d]­pyrimidine derivative SI306, a c-Src inhibitor....

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Published in:ACS medicinal chemistry letters 2020-05, Vol.11 (5), p.664-670
Main Authors: Molinari, Alessio, Iovenitti, Giulia, Mancini, Arianna, Gravina, Giovanni Luca, Chebbi, Monia, Caruana, Maura, Vignaroli, Giulia, Orofino, Francesco, Rango, Enrico, Angelucci, Adriano, Dreassi, Elena, Schenone, Silvia, Botta, Maurizio
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Language:English
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Letter
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Summary:Gold-nanoparticle (AuNP)-conjugated drugs represent a promising and innovative antitumor therapeutic approach. In our study, we describe the design, the synthesis, the preparation, and the characterization of AuNPs conjugated with the pyrazolo­[3,4-d]­pyrimidine derivative SI306, a c-Src inhibitor. AuNPs–SI306 showed a good loading efficacy (65%), optimal stability in polar media and in human plasma, and a suitable morphological profile: a ζ-potential of −43.9 mV, a nanoparticle diameter of 48.6 nm, and a 0.441 PDI value. The antitumoral activity of AuNPs–SI306 was evaluated in vitro in the glioblastoma model, by the low-density growth assay, and also in combination with radiotherapy (RT). Results demonstrated that AuNPs had a basal radiosensitization ability and that AuNPs–SI306, when used in combination with RT, were more effective in inhibiting tumor cell growth with respect to AuNPs and free SI306.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.9b00538