Synthesis and evaluation of (18)F-labeled ATP competitive inhibitors of topoisomerase II as probes for imaging topoisomerase II expression

Type II topoisomerase (Topo-II) is an ATP-dependent enzyme that is essential in the transcription, replication, and chromosome segregation processes and, as such, represents an attractive target for cancer therapy. Numerous studies indicate that the response to treatment with Topo-II inhibitors is h...

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Veröffentlicht in:	European journal of medicinal chemistry 2014-10, Vol.86, p.769
Hauptverfasser:	Daumar, Pierre, Zeglis, Brian M, Ramos, Nicholas, Divilov, Vadim, Sevak, Kuntal Kumar, Pillarsetty, NagaVaraKishore, Lewis, Jason S
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine Triphosphate - antagonists & inhibitors Adenosine Triphosphate - metabolism Animals Antigens, Neoplasm - metabolism Antineoplastic Agents - analysis Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Cell Proliferation - drug effects DNA Topoisomerases, Type II - metabolism DNA-Binding Proteins - antagonists & inhibitors DNA-Binding Proteins - metabolism Dose-Response Relationship, Drug Drug Screening Assays, Antitumor Fluorine Radioisotopes Humans MCF-7 Cells Mice Mice, SCID Molecular Imaging - methods Molecular Structure Neoplasms, Experimental - drug therapy Neoplasms, Experimental - enzymology Neoplasms, Experimental - pathology Positron-Emission Tomography Structure-Activity Relationship Topoisomerase II Inhibitors - analysis Topoisomerase II Inhibitors - chemical synthesis Topoisomerase II Inhibitors - chemistry Topoisomerase II Inhibitors - pharmacology Tumor Cells, Cultured
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