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Recent Advances in the Synthesis of Acyclic Nucleosides and Their Therapeutic Applications 无环核苷合成及其治疗应用的最新进展。
IF 8.6 2区 化学 Q1 Chemistry Pub Date : 2024-10-23 DOI: 10.1007/s41061-024-00476-7
Sumit Kumar, Aditi Arora, Riya Chaudhary, Rajesh Kumar, Christophe Len, Monalisa Mukherjee, Brajendra K. Singh, Virinder S. Parmar

DNA is commonly known as the “molecule of life” because it holds the genetic instructions for all living organisms on Earth. The utilization of modified nucleosides holds the potential to transform the management of a wide range of human illnesses. Modified nucleosides and their role directly led to the 2023 Nobel prize. Acyclic nucleosides, due to their distinctive physiochemical and biological characteristics, rank among the most adaptable modified nucleosides in the field of medicinal chemistry. Acyclic nucleosides are more resistant to chemical and biological deterioration, and their adaptable acyclic structure makes it possible for them to interact with various enzymes. A phosphonate group, which is linked via an aliphatic functionality to a purine or a pyrimidine base, distinguishes acyclic nucleoside phosphonates (ANPs) from other nucleotide analogs. Acyclic nucleosides and their derivatives have demonstrated various biological activities such as anti-viral, anti-bacterial, anti-cancer, anti-microbial, etc. Ganciclovir, Famciclovir, and Penciclovir are the acyclic nucleoside-based drugs approved by FDA for the treatment of various diseases. Thus, acyclic nucleosides are extremely useful for generating a variety of unique bioactive chemicals. Their biological activities as well as selectivity is significantly influenced by the stereochemistry of the acyclic nucleosides because chiral acyclic nucleosides have drawn a lot of interest due to their intriguing biological functions and potential as medicines. For example, tenofovir's (R) enantiomer is roughly 50 times more potent against HIV than its (S) counterpart. We can confidently state, “The most promising developments are yet to come in the realm of acyclic nucleosides!” Herein, we have covered the most current developments in the field of chemical synthesis and therapeutic applications of acyclic nucleosides based upon our continued interest and activity in this field since mid-1990’s.

Graphical Abstract

DNA 通常被称为 "生命分子",因为它掌握着地球上所有生物的遗传指令。利用改性核苷有望改变人类多种疾病的治疗方法。修饰核苷及其作用直接导致了 2023 年诺贝尔奖的产生。无环核苷具有独特的理化和生物学特性,是药物化学领域适应性最强的修饰核苷之一。无环核苷具有更强的抗化学和生物劣化能力,其适应性强的无环结构使其能够与各种酶相互作用。膦酸基通过脂肪族官能团与嘌呤或嘧啶碱基相连,是无环核苷膦酸盐(ANPs)与其他核苷酸类似物的区别所在。无环核苷及其衍生物具有多种生物活性,如抗病毒、抗菌、抗癌、抗微生物等。更昔洛韦(Ganciclovir)、泛昔洛韦(Famciclovir)和喷昔洛韦(Penciclovir)是 FDA 批准用于治疗各种疾病的无环核苷类药物。因此,无环核苷在生成各种独特的生物活性化学物质方面非常有用。无环核苷的立体化学对其生物活性和选择性有很大影响,因为手性无环核苷具有引人入胜的生物功能和作为药物的潜力,因此引起了广泛的兴趣。例如,替诺福韦的对映体(R)对艾滋病病毒的药效大约是其对映体(S)的50倍。我们可以自信地说:"无环核苷领域最有前途的发展还在后面!"自 1990 年代中期以来,我们一直关注无环核苷的化学合成和治疗应用领域,并在此基础上介绍了这一领域的最新进展。
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引用次数: 0
The Benzoxazole Heterocycle: A Comprehensive Review of the Most Recent Medicinal Chemistry Developments of Antiproliferative, Brain-Penetrant, and Anti-inflammatory Agents 苯并恶唑杂环:抗增殖、脑穿透和抗炎药物的最新药物化学发展综述
IF 8.6 2区 化学 Q1 Chemistry Pub Date : 2024-10-21 DOI: 10.1007/s41061-024-00477-6
Simona Di Martino, Maria De Rosa

The benzoxazole is one of the most widely exploited heterocycles in drug discovery. Natural occurring and synthetic benzoxazoles show a broad range of biological activities. Many benzoxazoles are available for treating several diseases, and, to date, a few are in clinical trials. Moreover, an ever-increasing number of benzoxazole derivatives are under investigation in the early drug discovery phase and as potential hit or lead compounds. This perspective is an attempt to thoroughly review the rational design, the structure–activity relationship, and the biological activity of the most notable benzoxazoles developed during the past 5 years (period 2019–to date) in cancers, neurological disorders, and inflammation. We also briefly overviewed each target and its role in the disease. The huge amount of work examined suggests the great potential of the scaffold and the high interest of the scientific community in novel biologically active compounds containing the benzoxazole core.

苯并恶唑是药物研发中应用最广泛的杂环之一。天然存在和合成的苯并恶唑具有广泛的生物活性。许多苯并噁唑类药物可用于治疗多种疾病,迄今为止,少数药物已进入临床试验阶段。此外,越来越多的苯并恶唑衍生物作为潜在的主打或先导化合物,正在药物发现的早期阶段接受研究。本视角试图全面回顾过去 5 年(2019 年至今)在癌症、神经系统疾病和炎症领域开发的最著名的苯并恶唑的合理设计、结构-活性关系和生物活性。我们还简要概述了每个靶点及其在疾病中的作用。所研究的大量工作表明了该支架的巨大潜力,以及科学界对含有苯并恶唑核心的新型生物活性化合物的浓厚兴趣。
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引用次数: 0
Unveiling the Significance of tert-Butoxides in Transition Metal-Free Cross-Coupling Reactions 揭示叔丁氧基在无过渡金属交叉偶联反应中的重要作用。
IF 8.6 2区 化学 Q1 Chemistry Pub Date : 2024-10-11 DOI: 10.1007/s41061-024-00478-5
Vipin Kumar, Suman Majee, Km. Anjali, Biswajit Saha, Devalina Ray

The astounding reactivity of tert-butoxides in transition metal-free coupling reactions is driving the scientific community towards a new era of environmental friendly, as well as cost-effective, transformation strategies. Transition metal-catalyzed coupling reactions generate hazardous wastes and require harsh reaction conditions, mostly at elevated temperature, which increases not only costs but also environmental concerns regarding the methodology. Tert-butoxide-catalyzed/mediated coupling reactions have several advantages and potential applications. They can form carbon–carbon, carbon–heteroatom, and heteroatom–heteroatom bonds under mild reaction conditions. Mechanistic insights into these reactions include both ionic and radical pathways, with the fate of the intermediates depending on the reaction conditions and/or additives used in the reactions. Among all of the known tert-butoxides, potassium tert-butoxide has pronounced applications in transition metal-free coupling reactions as compared to other tert-butoxides, such as sodium and lithium tert-butoxides, because of the higher electropositivity of potassium compared to sodium and lithium. Moreover, potassium tert-butoxide can act as a source of base, nucleophile and single electron donors in various important transformations. In this review, we provide an extensive overview and complete compilation of transition metal-free cross-coupling reactions catalyzed/promoted by tert-butoxides during the past 10 years.

Graphical Abstract

Tert-butoxide-mediated/activated cross-coupling reactions under the transition metal-free condition for benign organic transformation using a greener approach.

叔丁氧化合物在无过渡金属偶联反应中惊人的反应活性正推动科学界迈向环境友好型、高成本效益转化策略的新时代。过渡金属催化的偶联反应会产生危险废物,而且需要苛刻的反应条件,主要是在高温下进行,这不仅增加了成本,也增加了对环境的担忧。叔丁氧催化/介导的偶联反应具有多项优势和潜在应用。它们可以在温和的反应条件下形成碳-碳键、碳-杂原子键和杂原子-杂原子键。这些反应的机理包括离子途径和自由基途径,中间产物的去向取决于反应条件和/或反应中使用的添加剂。在所有已知的叔丁氧化合物中,与钠和锂叔丁氧化合物等其他叔丁氧化合物相比,叔丁醇钾在无过渡金属偶联反应中具有明显的应用优势,因为与钠和锂相比,钾具有更高的正电性。此外,叔丁醇钾还可以在各种重要的转化过程中充当碱源、亲核剂和单电子供体。在这篇综述中,我们对过去 10 年中由叔丁氧钾催化/促进的无过渡金属交叉偶联反应进行了广泛概述和完整汇编。
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引用次数: 0
Research Progress of Deep-Red to Near-Infrared Electroluminescent Materials Based on Organic Cyclometallated Platinum(II) Complexes 基于有机环金属化铂(II)配合物的深红至近红外电致发光材料的研究进展。
IF 8.6 2区 化学 Q1 Chemistry Pub Date : 2024-10-09 DOI: 10.1007/s41061-024-00479-4
Cheng Zhang, Yuanyuan Fang, Danfeng He, Keyue Xu, Yuzhu Bian, Yiru Li, Mingsheng Peng, Wenjing Xiong

In recent years, the near-infrared (NIR) light-emitting materials have attracted increasing attention due to the broad application prospects in the fields of military industry, aerospace, lighting, display and wearable devices. As the transition metal complexes, platinum(II) complexes have been shown to emit luminescence efficiently in NIR organic light-emitting diodes because of the unique d8 electron structure. This structure ensures that the platinum(II) complex molecules exhibit a high planarity, variety of excited states, and strong intermolecular interactions. This review summarizes the research progress of deep red to NIR organic light-emitting materials based on platinum(II) complexes in recent years and provides a certain reference for the further design and synthesis of NIR platinum(II) complex luminescent materials with superior performance.

近年来,近红外(NIR)发光材料因其在军工、航空航天、照明、显示和可穿戴设备等领域的广阔应用前景而受到越来越多的关注。作为过渡金属配合物,铂(II)配合物因其独特的 d8 电子结构,已被证明能在近红外有机发光二极管中高效发光。这种结构确保了铂(II)配合物分子具有高度的平面性、多种激发态和较强的分子间相互作用。本综述总结了近年来基于铂(II)配合物的深红至近红外有机发光材料的研究进展,为进一步设计和合成性能优越的近红外铂(II)配合物发光材料提供了一定的参考。
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引用次数: 0
Recent Focuses in the Syntheses and Applications of Magnetic Metal–Organic Frameworks 磁性金属有机框架的合成与应用的最新焦点。
IF 8.6 2区 化学 Q1 Chemistry Pub Date : 2024-10-06 DOI: 10.1007/s41061-024-00475-8
Yosra Mostafapour Kandelous, Mohammad Nikpassand, Leila Zare Fekri

In this article, we examine the recent uses of magnetic metal–organic frameworks (MMOFs). MMOFs can be used in various fields such as water purification, laboratory, food, environment, etc. Their materials can be composed of different metals and ligands, each of which has its own properties. Also, the presence of a magnetic property in these absorbents adds good features such as easy separation, faster absorption, and better interaction with other particles, which improves their application and performance. In recent years, various types of these compounds have been made, and, in this article, while classifying them, we will discuss the structure and application of some MMOFs.

Graphical Abstract

本文将探讨磁性金属有机框架(MMOFs)的最新用途。磁性金属有机框架可用于水净化、实验室、食品、环境等多个领域。它们的材料可以由不同的金属和配体组成,每种金属和配体都有自己的特性。此外,磁性吸附剂还具有易于分离、吸附速度更快、与其他颗粒的相互作用更强等优点,从而提高了其应用和性能。近年来,人们制造出了各种类型的此类化合物,本文在对它们进行分类的同时,将讨论一些 MMOF 的结构和应用。
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引用次数: 0
A Review on Recent Development of Phenothiazine-Based Chromogenic and Fluorogenic Sensors for the Detection of Cations, Anions, and Neutral Analytes 用于检测阳离子、阴离子和中性分析物的吩噻嗪基生色和生氟传感器的最新发展综述。
IF 8.6 2区 化学 Q1 Chemistry Pub Date : 2024-09-05 DOI: 10.1007/s41061-024-00474-9
Mohan Ilakiyalakshmi, Kumudhavalli Dhanasekaran, Ayyakannu Arumugam Napoleon

This review provides an in-depth examination of recent progress in the development of chemosensors, with a particular emphasis on colorimetric and fluorescent probes. It systematically explores various sensing mechanisms, including metal-to-ligand charge transfer (MLCT), ligand-to-metal charge transfer (LMCT), photoinduced electron transfer (PET), intramolecular charge transfer (ICT), and fluorescence resonance energy transfer (FRET), and elucidates the mechanism of action for cation and anion chemosensors. Special attention is given to phenothiazine-based fluorescence probes, highlighting their exceptional sensitivity and rapid detection abilities for a broad spectrum of analytes, including cations, anions, and small molecules. Phenothiazine chemosensors have emerged as versatile tools widely employed in a multitude of applications, spanning environmental and biomedical fields. Furthermore, it addresses existing challenges and offers insights into future research directions, aiming to facilitate the continued advancement of phenothiazine-based fluorescent probes.

Graphical Abstract

这篇综述深入探讨了化学传感器研发的最新进展,尤其侧重于比色和荧光探针。它系统地探讨了各种传感机制,包括金属-配体电荷转移(MLCT)、配体-金属电荷转移(LMCT)、光诱导电子转移(PET)、分子内电荷转移(ICT)和荧光共振能量转移(FRET),并阐明了阳离子和阴离子化学传感器的作用机制。该研究特别关注基于吩噻嗪的荧光探针,强调了它们对包括阳离子、阴离子和小分子在内的多种分析物的超高灵敏度和快速检测能力。吩噻嗪化学传感器已成为广泛应用于环境和生物医学领域的多功能工具。此外,该书还探讨了现有的挑战,并对未来的研究方向提出了见解,旨在促进基于吩噻嗪的荧光探针的持续发展。
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引用次数: 0
Emerging Nanomaterials as Versatile Nanozymes: A New Dimension in Biomedical Research 作为多功能纳米酶的新兴纳米材料:生物医学研究的新维度。
IF 8.6 2区 化学 Q1 Chemistry Pub Date : 2024-08-14 DOI: 10.1007/s41061-024-00473-w
Evin Jacob, Denno Mathew, Libina Benny, Anitha Varghese

The enzyme-mimicking nature of versatile nanomaterials proposes a new class of materials categorized as nano-enzymes, ornanozymes. They are artificial enzymes fabricated by functionalizing nanomaterials to generate active sites that can mimic enzyme-like functions. Materials extend from metals and oxides to inorganic nanoparticles possessing intrinsic enzyme-like properties. High cost, low stability, difficulty in separation, reusability, and storage issues of natural enzymes can be well addressed by nanozymes. Since 2007, more than 100 nanozymes have been reported that mimic enzymes like peroxidase, oxidase, catalase, protease, nuclease, hydrolase, superoxide dismutase, etc. In addition, several nanozymes can also exhibit multi-enzyme properties. Vast applications have been reported by exploiting the chemical, optical, and physiochemical properties offered by nanozymes. This review focuses on the reported nanozymes fabricated from a variety of materials along with their enzyme-mimicking activity involving tuning of materials such as metal nanoparticles (NPs), metal-oxide NPs, metal–organic framework (MOF), covalent organic framework (COF), and carbon-based NPs. Furthermore, diverse applications of nanozymes in biomedical research are discussed in detail.

多功能纳米材料的仿酶特性提出了一类新材料,即纳米酶(ornanozymes)。它们是通过对纳米材料进行功能化处理而制造出的人造酶,可产生模仿酶功能的活性位点。这些材料从金属和氧化物到无机纳米粒子都具有类似酶的内在特性。纳米酶可以很好地解决天然酶的高成本、低稳定性、难以分离、可重复使用和储存等问题。自 2007 年以来,已有 100 多种纳米酶被报道,它们模仿过氧化物酶、氧化酶、过氧化氢酶、蛋白酶、核酸酶、水解酶、超氧化物歧化酶等酶。此外,一些纳米酶还具有多酶特性。利用纳米酶的化学、光学和理化特性,已有大量应用报道。本综述将重点介绍已报道的由多种材料制成的纳米酶,以及它们的酶模拟活性,其中涉及对金属纳米颗粒(NPs)、金属氧化物 NPs、金属有机框架(MOF)、共价有机框架(COF)和碳基 NPs 等材料的调整。此外,还详细讨论了纳米酶在生物医学研究中的各种应用。
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引用次数: 0
The Hamilton Receptor in Supramolecular Polymer Sciences 超分子聚合物科学中的汉密尔顿受体。
IF 8.6 2区 化学 Q1 Chemistry Pub Date : 2024-07-20 DOI: 10.1007/s41061-024-00471-y
Shafieq Ahmad Wagay, Rashid Ali

Supramolecular polymers are polymeric materials of monomeric fragments, held jointly by reversible and directional non-covalent interactions such as multiple hydrogen-bonding, charge transfer effects, host–guest interactions, metal coordination, and aromatic stacking. This review article on the Hamilton-based supramolecular polymers aims to shed light on the molecular recognition achievements by the Hamilton-based polymeric systems, evaluate Hamilton receptor’s future prospects, and capitalize its potential applications in supramolecular chemistry. To the best of our knowledge, this is the first elaborative and sole manuscript in which polymeric Hamilton receptors are being exposed in detail. The first portion of this manuscript is related to the importance and urgency of polymers along with the historic background of Hamilton receptors. The middle section discloses the potential applications of Hamilton-type receptors in various fields, e.g., dendrimers, mechanically polymeric rotaxanes, and self-assemblies. The final section of the manuscript discloses the future aspects and the importance of novel polymer-based Hamilton-type receptors in the modern era. We believe that this first review in this emerging yet immature field will be useful to inspire scientists around the world to find the unseen future prospects, thereby boosting the field related to this valued artificial receptor in the province of supramolecular chemistry and also in other domains of scientific fields and technology, as well.

Graphical Abstract

超分子聚合物是由单体片段组成的高分子材料,通过可逆和定向的非共价相互作用,如多重氢键、电荷转移效应、主客体相互作用、金属配位和芳香堆积等,将单体片段联合在一起。这篇关于汉密尔顿基超分子聚合物的综述文章旨在揭示汉密尔顿基聚合物体系的分子识别成果,评估汉密尔顿受体的未来前景,以及其在超分子化学中的潜在应用。据我们所知,这是第一篇详细介绍聚合物汉密尔顿受体的手稿,也是唯一一篇详细介绍聚合物汉密尔顿受体的手稿。手稿的第一部分介绍了聚合物的重要性和紧迫性以及汉密尔顿受体的历史背景。中间部分介绍了汉密尔顿受体在各个领域的潜在应用,如树枝状聚合物、机械聚合物轮烷和自组装。手稿的最后一部分介绍了基于新型聚合物的汉密尔顿型受体在当代的前景和重要性。我们相信,这篇在这一新兴但尚不成熟领域的首次综述将有助于启发世界各地的科学家去寻找未知的未来前景,从而推动超分子化学领域以及其他科学领域和技术领域与这一有价值的人工受体相关的领域的发展。
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引用次数: 0
Review on Synthesis of 2-(2-Hydroxyaryl) Benzothiazoles (HBT) for Excited-State Intra-molecular Proton Transfer (ESIPT)-Based Detection of Ions and Biomolecules 基于激发态分子内质子转移 (ESIPT) 的离子和生物大分子检测的 2-(2-羟基芳基) 苯并噻唑 (HBT) 的合成综述。
IF 8.6 2区 化学 Q1 Chemistry Pub Date : 2024-07-18 DOI: 10.1007/s41061-024-00472-x
Amandeep Kaur, R. P. Chaudhary

In this review, we present a systematic and comprehensive summary of the recent developments in the synthetic strategies of 2-(2-hydroxyarylsubstituted)-benzothiazole (HBT) framework along with incorporation of various substituents on phenolic and benzothiazole rings which affect the emission process. The literature, spanning the years 2015–2024, on excited-state intramolecular proton transfer (ESIPT)-based studies of HBT derivatives comprising the effects of solvent polarity, substituents, and extended conjugation on fluorophores has been searched. ESIPT, intramolecular charge transfer, and aggregation-induced emissions enable these fluorescent probes to specifically interact with analytes, thereby altering their luminescence characteristics to achieve analyte detection. These fluorescent probes exhibit large Stokes shifts, high quantum yields, and excellent color transitions. Finally, the applications of HBTs as ESIPT-based fluorescent probes for the detection of cations, anions, and biomolecules have been summarized. We anticipate that this review will provide a comprehensive overview of the current state of research in this field and encourage researchers to develop novel ESIPT-based fluorophores with new applications.

在这篇综述中,我们系统而全面地总结了 2-(2-羟基芳基取代)-苯并噻唑(HBT)框架合成策略的最新进展,以及在酚醛环和苯并噻唑环上加入各种取代基对发射过程的影响。我们搜索了 2015-2024 年间基于激发态分子内质子转移(ESIPT)研究 HBT 衍生物的文献,包括溶剂极性、取代基和扩展共轭对荧光团的影响。ESIPT、分子内电荷转移和聚集诱导发射使这些荧光探针能够与分析物发生特异性相互作用,从而改变其发光特性,实现分析物检测。这些荧光探针具有较大的斯托克斯位移、较高的量子产率和出色的颜色转换。最后,我们总结了 HBT 作为基于 ESIPT 的荧光探针在检测阳离子、阴离子和生物分子方面的应用。我们希望这篇综述能全面概述该领域的研究现状,并鼓励研究人员开发基于 ESIPT 的新型荧光探针,以实现新的应用。
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引用次数: 0
Advances in Black Phosphorus Quantum Dots for Cancer Research: Synthesis, Characterization, and Applications 用于癌症研究的黑磷量子点的进展:合成、表征和应用》。
IF 8.6 2区 化学 Q1 Chemistry Pub Date : 2024-07-15 DOI: 10.1007/s41061-024-00470-z
Elham Einafshar, Ahmad Ghorbani

In the past few years, there has been notable advancement in nanotechnology, leading to the development of new materials with potential uses in the medical field, especially in cancer diagnosis, imaging, and therapy. Black phosphorus quantum dots (BPQDs) are one of the emerging nanomaterials that have generated interest due to their unique properties and potential in biomedical applications. This review aims to give a detailed overview of how BPQDs are synthesized, characterized, and utilized. The synthesis methods of BPQDs are discussed, with a focus on obtaining size-controlled and high-quality BPQDs. Two main approaches, top-down exfoliation and bottom-up techniques, are described. Despite advancements in synthesis, there are challenges hindering the practical application of BPQDs, such as poor dispersion and short durability. To address these issues, techniques to enhance biocompatibility and reduce potential toxicity, such as surface modifications, are discussed. BPQDs have potential in bioimaging as they offer higher resolution and sensitivity compared with traditional imaging agents. Their small size and expansive surface area make them suitable for drug delivery systems, enabling the effective incorporation of therapeutic substances. By functionalizing BPQDs with targeting ligands, they can selectively bind to cancer cells or tissue, making them ideal for targeted therapies. Moreover, BPQDs can serve as biosensors to detect biomarkers in bodily fluids, further expanding their biomedical applications. However, before they can be successfully translated into clinical settings, further research is needed to optimize the synthesis methods of BPQDs and evaluate their long-term safety profiles. Nonetheless, with ongoing research and development, the medical uses of BPQDs are expected to expand.

Graphic Abstract

在过去的几年里,纳米技术取得了显著的进步,开发出了在医疗领域,尤其是癌症诊断、成像和治疗方面具有潜在用途的新材料。黑磷量子点(BPQDs)是新兴的纳米材料之一,因其独特的性质和在生物医学领域的应用潜力而备受关注。本综述旨在详细介绍如何合成、表征和利用 BPQDs。文章讨论了 BPQDs 的合成方法,重点是如何获得尺寸可控的高质量 BPQDs。介绍了两种主要方法,即自上而下的剥离和自下而上的技术。尽管合成技术不断进步,但 BPQDs 的实际应用仍面临一些挑战,如分散性差和耐久性短。为了解决这些问题,我们讨论了增强生物相容性和降低潜在毒性的技术,如表面修饰。与传统成像剂相比,BPQDs 具有更高的分辨率和灵敏度,因此具有生物成像的潜力。BPQDs 体积小、表面积大,因此适合用于药物输送系统,能够有效地将治疗物质融入其中。通过用靶向配体对 BPQDs 进行功能化,它们可以选择性地与癌细胞或组织结合,从而成为靶向疗法的理想选择。此外,BPQDs 还可作为生物传感器检测体液中的生物标记物,进一步拓展其生物医学应用。不过,在成功应用于临床之前,还需要进一步研究优化 BPQDs 的合成方法并评估其长期安全性。尽管如此,随着研究和开发的不断深入,BPQDs 的医疗用途有望扩大。
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引用次数: 0
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Topics in Current Chemistry
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