Synthesis and preliminary evaluation of a novel glutamine derivative: (2S, 4S)4-[18F]FEBGln

被引：8

作者：

Huang, Yong ^{[1
]}

Liu, Song ^{[1
]}

Wu, Renbo ^{[1
]}

Zhang, Lifang ^{[2
]}

Zhang, Yan ^{[2
]}

Hong, Haiyan ^{[2
]}

Zhang, Aili ^{[2
]}

Xiao, Hao ^{[1
]}

Liu, Yajing ^{[1
]}

Wu, Zehui ^{[1
]}

Zhu, Lin ^{[2
]}

Kung, Hank F. ^{[1
,3
]}

机构：

[1] Capital Med Univ, Beijing Inst Brain Disorders, Beijing 100069, Peoples R China

[2] Beijing Normal Univ, Coll Chem, Beijing 100875, Peoples R China

[3] Univ Penn, Dept Radiol, Philadelphia, PA 19104 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2019年 / 29卷 / 09期

基金：

中国国家自然科学基金; 北京市自然科学基金;

关键词：

Glutamine; Synthesis; Transporter; Radiosynthesis; Amino acid; POSITRON-EMISSION-TOMOGRAPHY; PROSTATE-CANCER DETECTION; AMINO-ACID TRANSPORTERS; O-(2-F-18-FLUOROETHYL)-L-TYROSINE PET; BIOLOGICAL EVALUATION; TUMOR; EXPRESSION; ASCT2; AVAILABILITY; GLIOMAS;

D O I：

10.1016/j.bmcl.2019.03.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We report the preparation of a novel glutamine derivative, (2S, 4S)-2,5-diamino-4-(4-(2-fluoroethoxy)benzyl)-5-oxopentanoic acid, (2S, 4S) 4-[F-18]FEBGln ([F-18]4), through efficient organic and radiosyntheses. In vitro assays of [F-18]4 using MCF-7 cells showed that it entered cells via multiple amino acid transporter systems including system L and ASC2 transporters but not through the system A transporter. [F-18]4 showed promising properties for tumor imaging and may serve as a lead compound for further optimizing and targeting the system L transporter associated with enhanced glutamine metabolism in cancer cells.

引用

页码：1047 / 1050

页数：4

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