Xanthene dyes for cancer imaging and treatment: A material odyssey

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Karaman O., Alkan G. A. , Kizilenis C., Akgul C. C. , Gunbas G.

COORDINATION CHEMISTRY REVIEWS, vol.475, pp.1-45, 2023 (SCI-Expanded)

  • Publication Type: Article / Article
  • Volume: 475
  • Publication Date: 2023
  • Doi Number: 10.1016/j.ccr.2022.214841
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Chemical Abstracts Core
  • Page Numbers: pp.1-45
  • Middle East Technical University Affiliated: Yes


Cancer is still among the leading health issues today, considering the cost, effectiveness, complexity of

detection/treatment modalities and survival rates. One of the most important criteria for higher survival

rates is the early and sensitive diagnosis of the disease that can direct the treatment modalities effec-

tively. Florescence imaging agents emerged as an important alternative due to the current state of the

art due to their spatial and temporal resolution, high sensitivity and selectivity, ease of modification

towards generating activatable agents, ease of operation, and low cost. In addition to imaging, light-

based treatment modality, photodynamic therapy (PDT), attained remarkable attention, as it is minimally

invasive and has fewer side effects compared to the current standard of care treatments. Even though flu-

orescence imaging and PDT have these significant advantages, light that needs to excite the agent has

limited penetration in tissues, hindering widespread utilization. Hybrid xanthene dyes, particularly ones

bearing silicon or phosphine oxide as the bridging unit of xanthene moiety, gained significant interest not

only due to their excellent photochemical properties in aqueous media, high fluorescence quantum yield,

photostability but also their proper absorption and emission maxima that allow for deep tissue imaging

and therapy. Here, the design and synthesis strategies, key photophysical properties, their application in

fluorescence imaging applications, and surprisingly limited utilization as PDT agents of hybrid xanthene

dyes that emerged in the last decade have been reviewed in detail.