Molecular‐Target‐Based Anticancer Photosensitizer: Synthesis and in vitro Photodynamic Activity of Erlotinib–Zinc(II) Phthalocyanine Conjugates |
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| Authors: | Dr Feng‐Ling Zhang Qi Huang Prof Jian‐Yong Liu Prof Ming‐Dong Huang Prof Jin‐Ping Xue |
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| Affiliation: | 1. Fujian Engineering Research Center for Drugs, Diagnoses and Treatment of Photodynamic Therapy, College of Chemistry, Fuzhou University, Fuzhou, Fujian, 350108 (P.R. China);2. Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou, Fujian, 350002 (China) |
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| Abstract: | Targeted photodynamic therapy is a new promising therapeutic strategy to overcome growing problems in contemporary medicine, such as drug toxicity and drug resistance. A series of erlotinib–zinc(II) phthalocyanine conjugates were designed and synthesized. Compared with unsubstituted zinc(II) phthalocyanine, these conjugates can successfully target EGFR‐overexpressing cancer cells owing to the presence of the small molecular‐target‐based anticancer agent erlotinib. All conjugates were found to be essentially non‐cytotoxic in the absence of light (up to 50 μM ), but upon illumination, they show significantly high photo‐cytotoxicity toward HepG2 cells, with IC50 values as low as 9.61–91.77 nM under a rather low light dose (λ=670 nm, 1.5 J cm?2). Structure–activity relationships for these conjugates were assessed by determining their photophysical/photochemical properties, cellular uptake, and in vitro photodynamic activities. The results show that these conjugates are highly promising antitumor agents for molecular‐target‐based photodynamic therapy. |
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| Keywords: | conjugates erlotinib molecular targeting photodynamic therapy phthalocyanine |
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