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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Design, synthesis, characterization of peripherally tetra-pyridine-triazole-substituted phthalocyanines and their inhibitory effects on cholinesterases (AChE/BChE) and carbonic anhydrases (hCA I, II and IX)
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Design, synthesis, characterization of peripherally tetra-pyridine-triazole-substituted phthalocyanines and their inhibitory effects on cholinesterases (AChE/BChE) and carbonic anhydrases (hCA I, II and IX)

机译：设计，合成，表征外围四吡啶 - 三唑 - 取代的酞菁及其对胆碱酯酶（ACHE / BCHE）和碳酸酐（HCA I，II和IX）的抑制作用

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摘要

In this study, phthalocyanine precursors (5 and 9) and 1,2,3-triazole-substituted metal-free and metallo phthalocyanines (9a-c) were designed and synthesized for the first time and evaluated in vitro for key molecular targets. The structures of the novel compounds were characterized via FT-IR, H-1/C-13 NMR, UV-Vis, and mass spectroscopy. The inhibitory activities of the compounds were tested against human carbonic anhydrase isoforms hCA I, II (cytosolic, ubiquitous isozymes), and IX (transmembrane, cancer-associated isozyme) and cholinesterases (AChE and BChE, which are associated with Alzheimer's disease). Among the three phthalocyanines and starting compounds, 9b showed the most interesting profile as a nanomolar selective inhibitor of hCA I (K-i = 37.2 nM) and 9c showed the most effective inhibitory effect on hCA II, IX, AChE and BChE (K-i = 41.9, 27.4, 5.8 and 45.8 nM, respectively). This study is also the first example of cancer-associated isozyme hCA IX inhibition by phthalocyanines.
机译：在该研究中，首次设计并合成了酞菁前体（5和9）和1,2,3-三唑取代的金属无金属和金属酞菁（9A-C），并在体外评估关键分子靶标。通过FT-IR，H-1 / C-13 NMR，UV-Vis和质谱表征新化合物的结构。将化合物的抑制活性针对人碳酸酐酶同种型HC 8，II（细胞溶质，普遍存在的同工）和IX（跨膜，癌症相关的同工酶）和胆碱酯酶（与阿尔茨海默病有关的胆碱酯酶）进行测试。在三种酞菁和起始化合物中，9B显示最有趣的轮廓作为HCA I（Ki = 37.2nm）的纳米olar选择性抑制剂，9C显示对HCA II，IX，ACHE和BCHE的最有效的抑制作用（Ki = 41.9，分别为27.4,5.8和45.8 nm）。该研究也是酞菁的癌症相关的同工学HCA IX抑制的第一个例子。

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