The mitochondria are essential for tumorigenesis and have been regarded as important targets in cancer chemotherapy.Herein,the mitochondria-targeted platinum(Ⅱ)complexes have been prepared.The introduction of the tri...The mitochondria are essential for tumorigenesis and have been regarded as important targets in cancer chemotherapy.Herein,the mitochondria-targeted platinum(Ⅱ)complexes have been prepared.The introduction of the triazole group with larger steric hindrance through post-click reaction converts the hybridization of carbon from sp to sp^(2),endowing the complexes with an orthogonally oriented ligand with restricted rotation and emission enhancement characteristics.Methylation of the triazolyl ligand has led to platinum(Ⅱ)complexes that can efficiently enter cancer cells and selectively accumulate in mitochondria,leading to significant enhancement in phosphorescence.In vivo anti-cancer investigations have demonstrated their distinct antitumor efficacy in substantial inhibition of tumor growth in breast cancer mice through dissipation of mitochondrial membrane potential,inducing apoptosis of tumor cell with negligibly systemic cytotoxicity.展开更多
基金supported by Zhejiang Provincial Natural Science Foundation of China(LR22B010001,LQ23B010001)the National Natural Science Foundation of China(22201057,21871297)+7 种基金the General Research Fund(GRF)grant from the Research Grants Council of the Hong Kong Special Administrative Region,People’s Republic of China(HKU17303421)the Collaborative Research Fund(CRF)(C7075-21G)Hangzhou Normal University(2021QDL001,2021QDL065)the West Lake Scholar Plan,the Hangzhou Leading Innovation and Entrepreneurship Team Project(TD2022001)the CAS-Croucher Funding Scheme for Joint Laboratory on Molecular Functional Materials for Electronics,Switching and Sensingsupport from Sun Yat-Sen UniversityThe University of Hong Kongthe Innovation Technology Commission to the State Key Laboratory of Synthetic Chemistry。
文摘The mitochondria are essential for tumorigenesis and have been regarded as important targets in cancer chemotherapy.Herein,the mitochondria-targeted platinum(Ⅱ)complexes have been prepared.The introduction of the triazole group with larger steric hindrance through post-click reaction converts the hybridization of carbon from sp to sp^(2),endowing the complexes with an orthogonally oriented ligand with restricted rotation and emission enhancement characteristics.Methylation of the triazolyl ligand has led to platinum(Ⅱ)complexes that can efficiently enter cancer cells and selectively accumulate in mitochondria,leading to significant enhancement in phosphorescence.In vivo anti-cancer investigations have demonstrated their distinct antitumor efficacy in substantial inhibition of tumor growth in breast cancer mice through dissipation of mitochondrial membrane potential,inducing apoptosis of tumor cell with negligibly systemic cytotoxicity.
