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新型8-氧代-8H-环戊[a]苊烯-7-腈作为实体瘤缺氧细胞长波长荧光标记物的合成与评价

Synthesis and evaluation of novel 8-oxo-8H-cyclopenta[a]acenaphthylene-7-carbonitriles as long-wavelength fluorescent markers for hypoxic cells in solid tumor.

作者信息

Liu Yan, Xu Yufang, Qian Xuhong, Xiao Yi, Liu Jianwen, Shen Liyun, Li Junhui, Zhang Yuanxing

机构信息

School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.

出版信息

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1562-6. doi: 10.1016/j.bmcl.2005.12.031. Epub 2006 Jan 5.

Abstract

Novel bioreductive and long-wavelength fluorescent markers for hypoxic cells in solid tumor, 9-isocyano-8H-acenaphtho[l,2-b]pyrrol-8-one with the side chain of 2-nitroimidazole, were designed, synthesized, and evaluated in V79 379A Chinese hamster cells in vitro. Compounds A(2) and A(4) showed good hypoxic-oxic fluorescence differential in vitro (V79 cells) by using fluorescence scan ascent.

摘要

用于实体瘤中缺氧细胞的新型生物还原和长波长荧光标记物,即带有2-硝基咪唑侧链的9-异氰基-8H-苊并[1,2-b]吡咯-8-酮,已被设计、合成并在体外的V79 379A中国仓鼠细胞中进行了评估。通过荧光扫描上升法,化合物A(2)和A(4)在体外(V79细胞)显示出良好的缺氧-有氧荧光差异。

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