Rational design of platinum(Ⅱ)complexes with orthogonally oriented triazolyl ligand with emission enhancement characteristics for cancer chemotherapy in vivo  

作　　者：Yeye Ai Zherui Zhang Yuexuan Fei Ruirong Ye Angela Sin-Yee Law Zong-Wan Mao Junqiu Liu Yongguang Li Vivian Wing-Wah Yam 

机构地区：[1]Key Laboratory of Organosilicon Chemistry and Material Technology of Ministry of Education,College of Material Chemistry and Chemical Engineering,Hangzhou Normal University,Hangzhou 311121,China [2]Institute of Molecular Functional Materials,State Key Laboratory of Synthetic Chemistry and Department of Chemistry,The University of Hong Kong,Hong Kong,China [3]School of Chemistry,Sun Yat-Sen University,Guangzhou 510275,China [4]State Key Laboratory of Supramolecular Structure and Materials,Jilin University,Changchun 130012,China

出　　处：《Science China Chemistry》2023年第10期2878-2884,共7页中国科学（化学英文版）

基　　金：supported by Zhejiang Provincial Natural Science Foundation of China(LR22B010001,LQ23B010001);the National Natural Science Foundation of China(22201057,21871297);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 Sensing;support from Sun Yat-Sen University;The University of Hong Kong;the Innovation Technology Commission to the State Key Laboratory of Synthetic Chemistry。

摘　　要：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.

关 键 词：platinum(Ⅱ)complexes post-click reaction emission enhancement mitochondria-targeting ANTITUMOR 

分 类 号：R914[医药卫生—药物化学] O641.4[医药卫生—药学]