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.

中文翻译：

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AuNP吡唑并[3,4-d]嘧啶纳米系统与放疗联合治疗胶质母细胞瘤。

金纳米粒子（AuNP）偶联药物代表了一种有前途的创新抗肿瘤治疗方法。在我们的研究中，我们描述了与c-Src抑制剂吡唑并[3,4-d]嘧啶衍生物SI306共轭的AuNP的设计，合成，制备和表征。AuNPs-SI306具有良好的加载效率（65％），在极性介质和人体血浆中的最佳稳定性以及合适的形态特征：ζ电位为-43.9 mV，纳米粒径为48.6 nm，PDI值为0.441 。在胶质母细胞瘤模型中，通过低密度生长测定以及结合放疗（RT）评估了AuNPs-SI306的抗肿瘤活性。结果表明AuNPs具有基础放射增敏能力，并且AuNPs-SI306与RT结合使用时，