1454772-95-2Relevant articles and documents
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.
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.
