基于介芳基卟啉和厄洛替尼的新型细胞毒性共轭物的 "点击 "合成

IF 1.8 4区化学 Q3 CHEMISTRY, MULTIDISCIPLINARY

Mendeleev Communications Pub Date : 2024-09-01 DOI:10.1016/j.mencom.2024.09.019

Yuliya S. Bortnevskaya , Viktoriya A. Malikova , Natalia Yu. Karpechenko , Natal’ya A. Bragina , Kseniya A. Zhdanova

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引用次数: 0

摘要

根据含双（4-叠氮苯基）卟啉酸锌衍生物和 N-（3-乙炔基苯基氨基）-6,7-双（2-甲氧基乙氧基）-喹唑啉之间的 "点击 "反应方案，合成了基于合成卟啉型四吡咯和小分子靶向酪氨酸激酶抑制剂厄洛替尼的新型光治疗剂。最终化合物及其前体被测试为潜在的光敏剂，用于靶向光动力疗法（PDT），共轭物对 NKE 细胞的光诱导细胞毒性 IC50 为 0.86 ± 0.017 μm，对 A431 细胞的 IC50 为 0.54 ± 0.011 μm。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

The ‘click’ synthesis of new cytotoxic conjugate based on meso-arylporphyrin and Erlotinib

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The ‘click’ synthesis of new cytotoxic conjugate based on meso-arylporphyrin and Erlotinib

New phototherapeutic agents based on synthetic porphyrin- type tetrapyrroles and small-molecule-targeted tyrosine kinase inhibitor Erlotinib have been synthesized based on the scheme involving ‘click’ reaction between bis(4- azidophenyl)-containing zinc porphyrinate derivative and N-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)- quinazoline. The final compound and its precursors were tested as potential photosensitizers for targeted photo- dynamic therapy (PDT), the conjugate having shown photoinduced cytotoxicity IC₅₀ for NKE cells 0.86 ± 0.017 μm and for A431 cells 0.54 ± 0.011 μm.

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来源期刊

Mendeleev Communications 化学-化学综合

CiteScore

3.00

自引率

21.10%

发文量

226

审稿时长

4-8 weeks

期刊介绍： Mendeleev Communications is the journal of the Russian Academy of Sciences, launched jointly by the Academy of Sciences of the USSR and the Royal Society of Chemistry (United Kingdom) in 1991. Starting from 1st January 2007, Elsevier is the new publishing partner of Mendeleev Communications. Mendeleev Communications publishes short communications in chemistry. The journal primarily features papers from the Russian Federation and the other states of the former USSR. However, it also includes papers by authors from other parts of the world. Mendeleev Communications is not a translated journal, but instead is published directly in English. The International Editorial Board is composed of eminent scientists who provide advice on refereeing policy.