Literature DB >> 20207538

Synthesis and biological evaluation of anti-1-amino-2-[18F]fluoro-cyclobutyl-1-carboxylic acid (anti-2-[18F]FACBC) in rat 9L gliosarcoma.

Weiping Yu1, Larry Williams, Vernon M Camp, Jeffrey J Olson, Mark M Goodman.   

Abstract

A new [(18)F] labeled amino acid anti-1-amino-2-[(18)F]fluoro-cyclobutyl-1-carboxylic acid 9 (anti-2-[(18)F]FACBC) was synthesized in 30% decay-corrected yield with high radiochemical purity over 99%. The cyclic sulfamidate precursor was very stable and highly reactive towards nucleophilic radiofluorination. Cell uptake assays with rat 9L gliosarcoma cells showed that [(18)F]9 was transported into tumor cells via multiple amino acid transport systems, including L and A systems. Biodistribution study in rats with intracranial 9L gliosarcoma tumors demonstrated that [(18)F]9 had a rapid and prolonged accumulation in tumors with 26:1 tumor to brain ratio at 120 min post-injection. In this model, [(18)F]9 is a potential PET tracer for brain tumor imaging. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20207538     DOI： 10.1016/j.bmcl.2010.02.048

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  6 in total

1.  Synthesis, uptake mechanism characterization and biological evaluation of (18)F labeled fluoroalkyl phenylalanine analogs as potential PET imaging agents.

Authors:  Limin Wang; Wenchao Qu; Brian P Lieberman; Karl Plössl; Hank F Kung
Journal:  Nucl Med Biol       Date:  2011-01       Impact factor: 2.408

2.  System a amino acid transport-targeted brain and systemic tumor PET imaging agents 2-amino-3-[(18)F]fluoro-2-methylpropanoic acid and 3-[(18)F]fluoro-2-methyl-2-(methylamino)propanoic acid.

Authors:  Weiping Yu; Jonathan McConathy; Jeffrey J Olson; Mark M Goodman
Journal:  Nucl Med Biol       Date:  2014-08-01       Impact factor: 2.408

Review 3.  The next generation of positron emission tomography radiopharmaceuticals in oncology.

Authors:  Samuel L Rice; Celeste A Roney; Pierre Daumar; Jason S Lewis
Journal:  Semin Nucl Med       Date:  2011-07       Impact factor: 4.446

4.  Synthesis and evaluation of 18F labeled alanine derivatives as potential tumor imaging agents.

Authors:  Limin Wang; Zhihao Zha; Wenchao Qu; Hongwen Qiao; Brian P Lieberman; Karl Plössl; Hank F Kung
Journal:  Nucl Med Biol       Date:  2012-04-26       Impact factor: 2.408

5.  Synthesis and evaluation of ¹⁸F labeled FET prodrugs for tumor imaging.

Authors:  Limin Wang; Brian P Lieberman; Karl Ploessl; Hank F Kung
Journal:  Nucl Med Biol       Date:  2013-10-09       Impact factor: 2.408

6.  Synthesis of enantiopure 18F-trifluoromethyl cysteine as a structure-mimetic amino acid tracer for glioma imaging.

Authors:  Shaoyu Liu; Hui Ma; Zhanwen Zhang; Liping Lin; Gongjun Yuan; Xiaolan Tang; Dahong Nie; Shende Jiang; Guang Yang; Ganghua Tang
Journal:  Theranostics       Date:  2019-01-30       Impact factor: 11.556
  6 in total

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