Radiohalogenated Prostate-Specific Membrane Antigen (PSMA)-Based Ureas as Imaging Agents for Prostate Cancer

被引：183

作者：

Chen, Ying ^{[1
]}

Foss, Catherine A. ^{[1
]}

Byun, Youngjoo ^{[1
]}

Nimmagadda, Sridhar ^{[1
]}

Pullambahatla, Mrudula ^{[1
]}

Fox, James J. ^{[1
]}

Castanares, Mark ^{[2
]}

Lupold, Shawn E. ^{[3
]}

Babich, John W. ^{[4
]}

Mease, Ronnie C. ^{[1
]}

Pomper, Martin G. ^{[1
,2
]}

机构：

[1] Johns Hopkins Med Inst, Russell H Morgan Dept Radiol & Radiol Sci, Baltimore, MD 21231 USA

[2] Johns Hopkins Med Inst, Dept Pharmacol & Mol Sci, Baltimore, MD 21231 USA

[3] Johns Hopkins Med Inst, Dept Urol, Baltimore, MD 21231 USA

[4] Mol Insight Pharmaceut Inc, Cambridge, MA 02142 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 24期

关键词：

D O I：

10.1021/jm801055h

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

To extend our development of new imaging agents targeting the prostate-specific membrane antigen (PSMA), we have used the versatile intermediate 2-[3-(5-amino-1-carboxy-pentyl)-ureido]-pentanedioic acid (Lys-C(O)-Glu), which allows ready incorporation of radiohalogens for single photon emission computed tomography (SPECT) and positron emission tomography (PET). We prepared 2-[3-[1-carboxy-5-(4-[I-125]iodobenzoylamino)-pentyl]-ureido]-pentanedioic acid ([I-125]3), 2-[3-[1-carboxy-5-(4-[F-18]fluoro-benzoylamino)-pentyl-ureido]-pentanedioic acid ([F-18]6), and 2-(3-[1-carboxy-5-[(5-[I-125]iodo-pyridine-3-carbonyl)-amino]-pentyl ureido)-pentanedioic acid ([I-125]8) in 65-80% (nondecay-corrected), 30-35% (decay corrected), and 59-75% (nondecay-corrected) radiochemical yields. Compound [I-125]3 demonstrated 8.8 +/- 4.7% injected close per gram (%ID/g) within PSMA(+) PC-3 PIP tumor at 30 min postinjection, which persisted, with clear delineation of the tumor by SPECT. similar tumor uptake values at early time points were demonstrated for [F-18]6 (using PET) and [I-125]8. Because of the many radiohalogenated moieties that call be attached via the e amino group, the intermediate Lys-C(O)-Glu is an attractive template upon which to develop new imaging agents for prostate cancer.

引用

页码：7933 / 7943

页数：11

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