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可作为诊疗剂的新型氟代糖基化卟啉的合成与表征

Synthesis and Characterization of Novel Fluoro-glycosylated Porphyrins that can be Utilized as Theranostic Agents.

作者信息

Arja Katriann, Elgland Mathias, Appelqvist Hanna, Konradsson Peter, Lindgren Mikael, Nilsson K Peter R

机构信息

Division of Chemistry Department of Physics, Chemistry and Biology Linköping University 581 83 Linköping Sweden.

Department of Physics Norwegian University of Science and Technology, NTNU 7491 Trondheim Norway.

出版信息

ChemistryOpen. 2018 May 18;7(7):495-503. doi: 10.1002/open.201800020. eCollection 2018 Jul.

Abstract

Small molecules with modalities for a variety of imaging techniques as well as therapeutic activity are essential, as such molecules render opportunities to simultaneously conduct diagnosis and targeted therapy, so called theranostics. In this regard, glycoporphyrins have proven useful as theranostic agents towards cancer, as well as noncancerous conditions. Herein, the synthesis and characterization of heterobifunctional glycoconjugated porphyrins with two different sugar moieties, a common monosaccharide at three sites, and a 2-fluoro-2-deoxy glucose (FDG) moiety at the fourth site are presented. The fluoro-glycoconjugated porphyrins exhibit properties for multimodal imaging and photodynamic therapy, as well as specificity towards cancer cells. We foresee that our findings might aid in the chemical design of heterobifunctional glycoconjugated porphyrins that could be utilized as theranostic agents.

摘要

具有适用于多种成像技术的模式以及治疗活性的小分子至关重要,因为此类分子为同时进行诊断和靶向治疗提供了机会,即所谓的治疗诊断学。在这方面,糖卟啉已被证明可作为针对癌症以及非癌性病症的治疗诊断剂。本文介绍了具有两种不同糖部分的异双功能糖缀合卟啉的合成与表征,其中三个位点为常见单糖,第四个位点为2-氟-2-脱氧葡萄糖(FDG)部分。含氟糖缀合卟啉具有多模态成像和光动力治疗的特性,以及对癌细胞的特异性。我们预计,我们的研究结果可能有助于异双功能糖缀合卟啉的化学设计,这些卟啉可用作治疗诊断剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d69/6031858/a330ef23baa2/OPEN-7-495-g006.jpg

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