36717-77-8Relevant articles and documents
Novel 99mTc labelled complexes with 2-nitroimidazole isocyanide: Design, synthesis and evaluation as potential tumor hypoxia imaging agents
Ruan, Qing,Zhang, Xuran,Lin, Xiao,Duan, Xiaojiang,Zhang, Junbo
, p. 988 - 994 (2018)
Radiolabelled 2-nitroimidazoles have been used for imaging hypoxia. With the aim of developing novel 99mTc radiotracers for imaging hypoxia, four novel 2-nitroimidazole isocyanide derivatives (2a, 2b, 2c, and 2d) were synthesized and radiolabelling was carried out for preparing their corresponding 99mTc complexes. These 99mTc complexes were stable in vitro and could exhibit good hypoxic selectivity. The partition coefficient results indicated that they were hydrophilic, and an evaluation of biodistribution in mice bearing S180 tumors indicated that all of the complexes could accumulate in the tumors. Among them, 99mTc-2c exhibited the highest tumor uptake and tumor/blood and tumor/muscle ratios at 2 h post-injection. Further, single photon emission computed tomography (SPECT) imaging studies indicated clear accumulation in tumors, suggesting that 99mTc-2c was a promising candidate for hypoxia imaging.
Real time detection of ESKAPE pathogens by a nitroreductase-triggered fluorescence turn-on probe
Xu, Shengnan,Wang, Qinghua,Zhang, Qingyang,Zhang, Leilei,Zuo, Limin,Jiang, Jian-Dong,Hu, Hai-Yu
supporting information, p. 11177 - 11180 (2017/10/17)
The identification of bacterial pathogens is the critical first step in conquering infection diseases. A novel turn-on fluorescent probe for the selective sensing of nitroreductase (NTR) activity and its initial applications in rapid, real-time detection and identification of ESKAPE pathogens have been reported.
Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates
Rami, Marouan,Dubois, Ludwig,Parvathaneni, Nanda-Kumar,Alterio, Vincenzo,Van Kuijk, Simon J. A.,Monti, Simona Maria,Lambin, Philippe,De Simone, Giuseppina,Supuran, Claudiu T.,Winum, Jean-Yves
, p. 8512 - 8520 (2013/12/04)
A series of nitroimidazoles incorporating sulfonamide/sulfamide/sulfamate moieties were designed and synthesized as radio/chemosensitizing agent targeting the tumor-associated carbonic anhydrase (CA) isoforms IX and XII. Most of the new compounds were nanomolar inhibitors of these isoforms. Crystallographic studies on the complex of hCA II with the lead sulfamide derivative of this series clarified the binding mode of this type of inhibitors in the enzyme active site cavity. Some of the best nitroimidazole CA IX inhibitors showed significant activity in vitro by reducing hypoxia-induced extracellular acidosis in HT-29 and HeLa cell lines. In vivo testing of the lead molecule in the sulfamide series, in cotreatment with doxorubicin, demonstrated a chemosensitization of CA IX containing tumors. Such CA inhibitors, specifically targeting the tumor-associated isoforms, are candidates for novel treatment strategies against hypoxic tumors overexpressing extracellular CA isozymes.
