Literature DB >> 19695886

A fully automated two-step synthesis of an (18)F-labelled tyrosine kinase inhibitor for EGFR kinase activity imaging in tumors.

D Kobus1, Y Giesen, R Ullrich, H Backes, B Neumaier.   

Abstract

Radiolabelled epidermal growth factor receptor (EGFR) tyrosine kinase (TK) inhibitors potentially facilitate the assessment of EGFR overexpression in tumors. Since elaborate multi-step radiosyntheses are required for (18)F-labelling of EGFR-specific anilinoquinazolines we report on the development of a two-step click labelling approach that was adapted to a fully automated synthesis module. 6-(4-N,N-Dimethylaminocrotonyl)amido-4-(3-chloro-4-fluoro)phenylamino-7-{3-[4-(2-[(18)F]fluoroethyl)-2,3,4-triazol-1-yl]propoxy}quinazoline ([(18)F]6) was synthesized via Huisgen 1,3-dipolar cycloaddition between 2-[(18)F]fluoroethylazide ([(18)F]4) and the alkyne modified anilinoquinazoline precursor 5. PET images of PC9 tumor xenograft using the novel biomarker showed promising results to visualize EGFR overexpression.

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Year:  2009        PMID： 19695886     DOI： 10.1016/j.apradiso.2009.07.018

Source DB:  PubMed          Journal:  Appl Radiat Isot        ISSN： 0969-8043            Impact factor:   1.513


  9 in total

Review 1.  Click Reaction: An Applicable Radiolabeling Method for Molecular Imaging.

Authors:  Ji Young Choi; Byung Chul Lee
Journal:  Nucl Med Mol Imaging       Date:  2015-10-19

Review 2.  18 F-Labeling of Sensitive Biomolecules for Positron Emission Tomography.

Authors:  Hema S Krishnan; Longle Ma; Neil Vasdev; Steven H Liang
Journal:  Chemistry       Date:  2017-09-01       Impact factor: 5.236

Review 3.  Click Chemistry and Radiochemistry: The First 10 Years.

Authors:  Jan-Philip Meyer; Pierre Adumeau; Jason S Lewis; Brian M Zeglis
Journal:  Bioconjug Chem       Date:  2016-11-22       Impact factor: 4.774

Review 4.  Plasticity of tumour and immune cells: a source of heterogeneity and a cause for therapy resistance?

Authors:  Michael Hölzel; Anton Bovier; Thomas Tüting
Journal:  Nat Rev Cancer       Date:  2013-03-28       Impact factor: 60.716

Review 5.  The application of click chemistry in the synthesis of agents with anticancer activity.

Authors:  Nan Ma; Ying Wang; Bing-Xin Zhao; Wen-Cai Ye; Sheng Jiang
Journal:  Drug Des Devel Ther       Date:  2015-03-12       Impact factor: 4.162

6.  Synthesis and pre-clinical evaluation of a new class of high-affinity 18F-labeled PSMA ligands for detection of prostate cancer by PET imaging.

Authors:  James Kelly; Alejandro Amor-Coarasa; Anastasia Nikolopoulou; Dohyun Kim; Clarence Williams; Shashikanth Ponnala; John W Babich
Journal:  Eur J Nucl Med Mol Imaging       Date:  2016-11-15       Impact factor: 9.236

Review 7.  Radiolabeled small molecule protein kinase inhibitors for imaging with PET or SPECT.

Authors:  Justin W Hicks; Henry F VanBrocklin; Alan A Wilson; Sylvain Houle; Neil Vasdev
Journal:  Molecules       Date:  2010-11-15       Impact factor: 4.411

Review 8.  18F-labeling using click cycloadditions.

Authors:  Kathrin Kettenbach; Hanno Schieferstein; Tobias L Ross
Journal:  Biomed Res Int       Date:  2014-05-27       Impact factor: 3.411

9.  Intermittent high-dose treatment with erlotinib enhances therapeutic efficacy in EGFR-mutant lung cancer.

Authors:  Jakob Schöttle; Sampurna Chatterjee; Caroline Volz; Maike Siobal; Alexandra Florin; Dennis Rokitta; Yvonne Hinze; Felix Dietlein; Dennis Plenker; Katharina König; Kerstin Albus; Johannes M Heuckmann; Daniel Rauh; Thomas Franz; Bernd Neumaier; Uwe Fuhr; Lukas C Heukamp; Roland T Ullrich
Journal:  Oncotarget       Date:  2015-11-17
  9 in total

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