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Manuscript CHEMRXIV.pdf (649.32 kB)
Tuning Organelle Specificity and Photodynamic Therapy Efficiency by Molecular Function Design
Preprints are manuscripts made publicly available before they have been submitted for formal peer review and publication. They might contain new research findings or data. Preprints can be a draft or final version of an author's research but must not have been accepted for publication at the time of submission.
submitted on 08.07.2019 and posted on 08.07.2019by zhiyang liu, hang zou, zheng zhao, Pengfei Zhang, Guogang shan, Ryan Tsz Kin Kwok, Jacky W. Y. Lam, Lei Zheng, Ben Zhong Tang
organic photosensitizers (PSs) have attracted much attention because of their
promising applications in photodynamic therapy (PDT). However, guidelines on
their molecular design are rarely reported. In this work, a series of PSs are
designed and synthesized based on a triphenylamine-azafluorenone core. Their
structure-property-application relationships are systematically studied.
Cationization is an effective strategy to enhance the PDT efficiency of PSs.
From the molecularly dispersed state to the aggregate state, the fluorescence
and the reactive oxygen species generation efficiency of PSs with
aggregation-induced emission (AIE) increase due to the restriction of the
intramolecular motions and enhancement of intersystem crossing. Cationized mitochondrion-targeting
PSs show higher PDT efficiency than that of nonionized ones targeting lipid
droplets. The ability of AIE PSs to kill cancer cells can be further enhanced
by combination of PDT with radiotherapy. Such results should trigger research
enthusiasm for designing and synthesizing new AIE PSs with better PDT
efficiency and new properties.