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    Online Resource
    Online Resource
    Future Science Ltd ; 2022
    In:  Future Medicinal Chemistry Vol. 14, No. 22 ( 2022-11), p. 1635-1647
    In: Future Medicinal Chemistry, Future Science Ltd, Vol. 14, No. 22 ( 2022-11), p. 1635-1647
    Abstract: Background: O-propyloxime-N-propoxybacteriopurpurinimide methyl ester (3) is a near-infrared photosensitizer with confirmed in vivo anticancer activity. Methods: Conjugates of 3 with arginine (1) or lysine attached at an ε-amino group (2a) or α-amino group (2b) were studied as anticancer and antibacterial photosensitizers and compared with 3. Results: The new conjugates preserve advanced spectral characteristics of 3 and high singlet oxygen quantum yield. They demonstrated tenfold higher photocytotoxicity for cancer cells, due to their enhanced intracellular accumulation and altered localization. Though they showed threefold decreased antibacterial photodynamic effect compared with 3, they kill planktonic Staphylococcus aureus bacteria, and 1 destroys bacterial biofilms. Conclusion: Conjugates 1 and 2b are near-infrared photosensitizers with high anticancer and limited antibacterial activity.
    Type of Medium: Online Resource
    ISSN: 1756-8919 , 1756-8927
    Language: English
    Publisher: Future Science Ltd
    Publication Date: 2022
    SSG: 15,3
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