DNA methyltransferase 1 fluorescent probe and application thereof

The invention belongs to the technical field of medicines, and relates to a DNA methyltransferase 1 fluorescent probe, in particular to a fluorescent probe formed by connecting a phthalimide DNA methyltransferase 1 (DNMT1) inhibitor and fluorescein through a connecting chain (L) and application of t...

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Hauptverfasser: RUAN MINLI, CHENG QUNXIAN, XU LING, ZHANG QIAN, GONG CHAOCHAO
Format: Patent
Sprache:chi ; eng
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Beschreibung
Zusammenfassung:The invention belongs to the technical field of medicines, and relates to a DNA methyltransferase 1 fluorescent probe, in particular to a fluorescent probe formed by connecting a phthalimide DNA methyltransferase 1 (DNMT1) inhibitor and fluorescein through a connecting chain (L) and application of the fluorescent probe. The fluorescent probe with the structure shown as the formula 1 or a pharmaceutically acceptable salt, a stereoisomer or a tautomer or a prodrug of the fluorescent probe shows good transmembrane nucleus entering capacity and DNMT1 binding capacity, can be used for preparing a quantitative detection preparation for DNMT1 in cells and cell nuclei, and provides prediction or diagnosis for cytopathy, especially the canceration degree. 本发明属医药技术领域,涉及DNA甲基转移酶1荧光探针,具体涉及式1结构的由邻苯二甲酰亚胺类DNA甲基转移酶1(DNMT1)抑制剂与荧光素通过连接链(L)连接而成的荧光探针及其用途。本发明式1结构的荧光探针,或其药学上可以接受的盐、其立体异构体或互变异构体、或前药,表现出良好的透膜入核能力和与DNMT1的结合能力,可用于制备细胞内及细胞核内的DNMT1的定量检测制剂,为细胞病变尤其是癌变程度提供预测或诊断。