1454772-97-4Relevant academic research and scientific papers
Molecular-target-based anticancer photosensitizer: Synthesis and in vitro photodynamic activity of erlotinib-zinc(II) phthalocyanine conjugates
Zhang, Feng-Ling,Huang, Qi,Liu, Jian-Yong,Huang, Ming-Dong,Xue, Jin-Ping
, p. 312 - 320 (2015/02/05)
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 mo-lecular- target-based anticancer agent erlotinib. All conjugates were found to be essentially non-cytotoxic in the absence of light (up to 50 mm), 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.
A novel strategy for targeting photodynamic therapy. Molecular combo of photodynamic agent zinc(II) phthalocyanine and small molecule target-based anticancer drug erlotinib
Zhang, Feng-Ling,Huang, Qi,Zheng, Ke,Li, Jun,Liu, Jian-Yong,Xue, Jin-Ping
supporting information, p. 9570 - 9572 (2013/10/08)
In this study, two phthalocyanine-erlotinib conjugates linked by an oligoethylene glycol chain have been synthesised and fully characterised. Having erlotinib as the targeting moiety, the two conjugates exhibited high specific affinity to HepG2 cancer cells and tumour tissues, therefore leading to high photodynamic activity. The Royal Society of Chemistry 2013.
