Design, radiosynthesis, and evaluation of radiotracers for positron emission tomography imaging of stearoyl-CoA desaturase-1

William C. Silvers, Hancheng Cai, Orhan K. Öz, Xiankai Sun

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

Design, radiosynthesis, and biological evaluation of two radiotracers (N-(3-[18F]fluoropropyl)-6-(4-(trifluoromethyl)benzoyl)-piperazin-1-yl)pyridazine-3-carboxamide (18F-FPPPT) and (N-(4-[18F]fluoroaniline)-6-(4-(trifluoromethyl)benzoyl)-piperazin-1-yl)pyridazine-3-carboxamide (18F-FAPPT)) are described for noninvasive assessment of stearoyl-CoA desaturase-1 (SCD-1). The overexpression of SCD-1 in multiple solid tumors associates with poor survival in cancer patients. The two radiotracers,18F-FPPPT and18F-FAPPT, were each prepared in three steps in radiochemical yields of 21% and 3%, respectively. The practicality of imaging SCD-1 with18F-FPPPT was tested in two mouse models bearing xenograft tumors with different levels of SCD-1 expression, which afforded a 1.8-fold uptake difference correspondingly. Our work indicates that it is possible to develop SCD-1 specific imaging probes from previously reported SCD-1 inhibitors.

Original languageEnglish (US)
Pages (from-to)924-927
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number3
DOIs
StatePublished - 2016

Fingerprint

Stearoyl-CoA Desaturase
Positron emission tomography
Positron-Emission Tomography
Imaging techniques
Tumors
Bearings (structural)
Neoplasms
Heterografts
Survival

Keywords

  • F-FPPPT
  • De novo lipid metabolism
  • PET
  • Radiosynthesis
  • Stearoyl-CoA desaturase

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Cite this

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title = "Design, radiosynthesis, and evaluation of radiotracers for positron emission tomography imaging of stearoyl-CoA desaturase-1",
abstract = "Design, radiosynthesis, and biological evaluation of two radiotracers (N-(3-[18F]fluoropropyl)-6-(4-(trifluoromethyl)benzoyl)-piperazin-1-yl)pyridazine-3-carboxamide (18F-FPPPT) and (N-(4-[18F]fluoroaniline)-6-(4-(trifluoromethyl)benzoyl)-piperazin-1-yl)pyridazine-3-carboxamide (18F-FAPPT)) are described for noninvasive assessment of stearoyl-CoA desaturase-1 (SCD-1). The overexpression of SCD-1 in multiple solid tumors associates with poor survival in cancer patients. The two radiotracers,18F-FPPPT and18F-FAPPT, were each prepared in three steps in radiochemical yields of 21{\%} and 3{\%}, respectively. The practicality of imaging SCD-1 with18F-FPPPT was tested in two mouse models bearing xenograft tumors with different levels of SCD-1 expression, which afforded a 1.8-fold uptake difference correspondingly. Our work indicates that it is possible to develop SCD-1 specific imaging probes from previously reported SCD-1 inhibitors.",
keywords = "F-FPPPT, De novo lipid metabolism, PET, Radiosynthesis, Stearoyl-CoA desaturase",
author = "Silvers, {William C.} and Hancheng Cai and {\"O}z, {Orhan K.} and Xiankai Sun",
year = "2016",
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T1 - Design, radiosynthesis, and evaluation of radiotracers for positron emission tomography imaging of stearoyl-CoA desaturase-1

AU - Silvers, William C.

AU - Cai, Hancheng

AU - Öz, Orhan K.

AU - Sun, Xiankai

PY - 2016

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