1454772-95-2Relevant 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)
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.
An epidermal growth factor receptor-targeted and endoplasmic reticulum-localized organic photosensitizer toward photodynamic anticancer therapy
Zhao, Xuan,Ma, Haixia,Chen, Juanjuan,Zhang, Fengling,Jia, Xiao,Xue, Jinping
, (2019/08/26)
The endoplasmic reticulum (ER), as the largest organelle in eukaryotic cells, plays complex but pivotal roles in multiple intracellular metabolic functions, including biosynthesis, sensing, and signal transduction, especially in proteins folding and post-translation modification. The ER is regarded as a promising target for anticancer therapy. Based on previous tumor-targeted photodynamic therapy (PDT), we chemically modified the phthalocyanine-based photosensitizer molecule with the small molecular anticancer-targeting drug erlotinib and the ER-targetable moiety methyl sulfonamide to develop an advanced photosensitizer EB-ER-Pc that can specifically target the subcellular organelle ER of EGFR-overexpressing cancer cells. The in vitro experiments show that the dual-target photosensitizer EB-ER-Pc can generate ROS in situ in the ER of the tumor target region to induce ER stress, upregulate Ca2+ ion level, and decrease mitochondrial membrane potential (MMP) to mediate cancer cells death and ablation. The results suggest that EB-ER-Pc is a promising candidate for effective photodynamic cancer therapy.
Preparation method and applications of photosensitizer targeting at EGFR excess expression tumor cell endoplasmic reticulum
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Paragraph 0020; 0025, (2019/10/01)
The invention discloses a photosensitizer targeting at EGFR excess expression tumor cell endoplasmic reticulum, and a preparation method thereof. According to the preparation method, phthalocyanine mother ring is connected with small molecular target medicine erlotinib(N-(3-acetylene phenyl)-[6, 7-di(2-methoxy ethoxy)] quinazoline-4-amine) through water soluble alcoxyl long chains in the axial direction through covalent bonds, so that the amphipathy, the bio-compatibility, and the selective targeting performance of the photosensitizer on tumor cells are improved; groups targeting at endoplasmic reticulum are introduced onto the other end of the phthalocyanine mother ring, so that, in vivo, the photosensitizer is capable of realizing selective targeting on endoplasmic reticulum, and photodynamic action efficiency is increased. The structure is single; the synthesis route is mature; the composition is determined; no isomer is generated; product separation and purification are convenient; and at the same time, aggregation of the complex is not easily caused, so that it is beneficial for increasing of cell uptake ratio.
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.
