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高度取代的噁唑衍生物作为细胞器靶向荧光团的细胞成像研究（OTFPs）。

Cell-imaging studies of highly substituted oxazole derivatives as organelle targeting fluorophores (OTFPs).

机构信息

Organic and Medicinal Chemistry Division, Indian Institute of Chemical Biology (CSIR-IICB), 4 Raja S. C. Mullick Road, Kolkata, 700032, India.

Cancer Biology & Inflammatory Disorder Division, Indian Institute of Chemical Biology (CSIR-IICB), 4 Raja S. C. Mullick Road, Kolkata, 700032, India.

出版信息

Sci Rep. 2022 Oct 3;12(1):16555. doi: 10.1038/s41598-022-20112-y.

DOI:10.1038/s41598-022-20112-y
PMID:36192545
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9530160/
Abstract

The field of biomedical science has progressed enormously in the past decade. With the advent of newer diagnostic tools for imaging and detection, identification of root cause of a disease is now remarkably accurate and specific. Small organic fluorophores in these connections are in great demand currently for cellular organelle sensing and detecting, due to their non-invasiveness, excellent accuracy and bio-sensitivity. Small molecule fluorescence probes offer most potent area for biological sensing with diagnostic imaging ability. These organelle targetable fluorescent probes are produced through synthetic manipulations to get the desired, decent fluorescence properties. When a suitable organelle specific functional group is installed within these highly fluorescent scaffolds, then these molecules turn out to be as lysotracker, mitotracker and cytoplasm-stainer in mammalian cells with high efficiencies (high Pearson co-efficient factors). The present work demonstrated an environmentally benign (green) one-pot, sp C-H functionalization of highly substituted oxazole derivatives with excellent photophysical properties. These molecules were further modified by installing organelle specific targetable groups (sensors/detectors) which selectively localize in specific intra-cellular organelles.

摘要

在过去的十年中，生物医学科学领域取得了巨大的进展。随着新型成像和检测诊断工具的出现，疾病的根本原因现在可以得到非常准确和具体的识别。由于其非侵入性、出色的准确性和生物敏感性，这些连接中的小分子荧光团目前对细胞细胞器的感应和检测有很大的需求。小分子荧光探针为具有诊断成像能力的生物感应提供了最有效的领域。这些细胞器靶向荧光探针是通过合成操作产生的，以获得所需的、良好的荧光特性。当在这些高荧光支架内安装合适的细胞器特异性功能基团时，这些分子就会成为哺乳动物细胞中的溶酶体追踪剂、线粒体追踪剂和细胞质染色剂，具有很高的效率（高皮尔逊相关系数因子）。本工作展示了一种环境友好的（绿色）一锅法 sp^C-H 官能化高度取代的恶唑衍生物，具有优异的光物理性质。这些分子进一步通过安装细胞器特异性靶向基团（传感器/探测器）进行修饰，这些基团可以选择性地定位于特定的细胞内细胞器。

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