期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 11, 期 5, 页码 664-670出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00538
关键词
Glioblastoma; Tyrosine kinase Src inhibitor; Nanotechnology; Gold nanoparticles; Radiotherapy
资金
- AIRC (Associazione Italiana per la Ricerca sul Cancro) [IG-2015, 17677]
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: zeta-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.
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