A Second Near-Infrared Ru(II) Polypyridyl Complex for Synergistic Chemo-Photothermal Therapy

Yishen Liu, Qianqian Li, Meijia Gu, Disheng Lu, Xiaoxing Xiong, Zhiyun Zhang, Yanna Pan, Yuqin Liao, Qihang Ding, Wanxia Gong, Dean Shuailin Chen, Mengting Guan, Junzhu Wu, Zhiquan Tian, Hai Deng, Lijuan Gu*, Xuechuan Hong, Yuling Xiao

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

27 Citations (Scopus)


The clinical success of cisplatin ushered in a new era of the application of metallodrugs. When it comes to practice, however, drug resistance, tumor recurrence, and drug systemic toxicity make it implausible to completely heal the patients. Herein, we successfully transform an electron acceptor [1, 2, 5]thiadiazolo[3,4-g]quinoxaline into a novel second near-infrared (NIR-II) fluorophore H7. After PEGylation and chelation, HL-PEG2k exhibits a wavelength bathochromic shift, enhanced photothermal conversion efficiency (41.77%), and an antineoplastic effect against glioma. Its potential for in vivo tumor tracking and image-guided chemo-photothermal therapy is explored. High levels of uptake and high-resolution NIR-II imaging results are thereafter obtained. The hyperthermia effect could disrupt the lysosomal membranes, which in turn aggravate the mitochondria dysfunction, arrest the cell cycle in the G2 phase, and finally lead to cancer cell apoptosis. HL-PEG2k displays a superior biocompatibility and thus can be a potential theranostic platform to combat the growth and recurrence of tumors.

Original languageEnglish
Pages (from-to)2225-2237
Number of pages13
JournalJournal of Medicinal Chemistry
Issue number3
Early online date7 Jan 2022
Publication statusPublished - 10 Feb 2022

Bibliographical note

Funding Information:
This work was supported by the National Key R&D Program of China (2020YFA0908800), NSFC (81773674, 81573383, 82111530209, and 91959103), Shenzhen Science and Technology Research Grant (JCYJ20190808152019182), Hubei Province Scientific and Technical Innovation Key Project (2020BAB058), the Natural Science Foundation of Hubei Province (Grant No. 2021CFB014), the Applied Basic Research Program of Wuhan Municipal Bureau of Science and Technology (2019020701011429), the Doctoral Foundation of Huanggang Normal University (2042021007 and 20420218704), Tibet Autonomous Region Science and Technology Plan Project Key Project (XZ201901-GB-11), the Local Development Funds of Science and Technology Department of Tibet (XZ202102YD0033C and XZ202001YD0028C), and the Fundamental Research Funds for the Central Universities.


  • Antineoplastic agents
  • Fluorescence
  • Lasers
  • Rodent models
  • Tumors


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