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Design, synthesis and biological evaluation of coumarin coupled nitroimidazoles as potential imaging agents

机译：香豆素偶联硝基咪唑作为潜在成像剂的设计，合成及生物学评价

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Solid tumors contain regions of hypoxia in comparison to normal tissues. The nitroimidazoles have shown great promise for targeting different types of cancers. The present work involves the design, syntheses, and in vitro and in vivo investigations of hypoxia targeted nitroimidazole radioconjugates (2NIHC and 4NIHC). Flow cytometry analysis showed that the normoxic-hypoxic mean fluorescence of 2NIHC is 10 fold greater than that of 4NIHC and much higher than that of the well-known pimonidazole hypoxia marker. Furthermore, molecular modeling studies of these ligands with CK2 alpha revealed that 2NIHC is a more potential CK2 alpha inhibitor due to pi-pi interactions and H-bonding with Val116, Glu114, Asp175, Asn161 and His160 in the active pockets of the target. Radio labeling yields for both the complexes with Tc-99m were > 98%. Biodistribution in EAT tumor bearing mice demonstrated rapid clearance of Tc-99m-2NIHC and high T/M ratio (3.57% ID/g) as compared to Tc-99m-4NIHC (2.05% ID/g) at 4 h. IC50 values of both ligands were estimated by MTS in different cell lines in addition to tumor regression studies.
机译：与正常组织相比，固体肿瘤含有缺氧的区域。 Nitroimidazoles对针对不同类型的癌症表现出了很好的希望。本作本作涉及设计，合成和体外和体内研究缺氧靶向硝基咪唑radioconjugates（2nihc和4nihc）。流式细胞术分析表明，2NIHC的常氧 - 缺氧平均荧光比4niHC的常倍数大，远高于众所周知的吡吡唑缺氧标记。此外，具有CK2α的这些配体的分子建模研究表明，由于PI-PI相互作用和与Val116，Glu114，Asp175，Asn161和His160的H键合，2niHC是一种更潜在的CK2α抑制剂。具有TC-99M的复合物的无线电标记产率> 98％。与TC-99M-4NIHC（2.05％ID / g）相比，Eat肿瘤轴承小鼠的肿瘤轴承小鼠的轴承小鼠的快速清除明确清除TC-99M-2NIHC和高T / M比率（3.57％ID / g）。除了肿瘤回归研究之外，不同细胞系中的MTS在不同细胞系中估计了两个配体的IC 50值。

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