Toward development of targeted nonsteroidal antiandrogen-1,4,7,10- tetraazacyclododecane-1,4,7,10-tetraacetic acid-gadolinium complex for prostate cancer diagnostics

Hanit Marom, Keren Miller, Yossi Bechor-Bar, Galia Tsarfaty, Ronit Satchi-Fainaro*, Michael Gozin

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

Abstract

Androgen receptors are present in most advanced prostate cancer specimens, having a critical role in development of this type of cancer. For correct prognosis of patient conditions and treatment monitoring, noninvasive imaging techniques have great advantages over surgical procedures. We developed synthetic methodologies for preparation of novel androgen receptor-targeting agents in an attempt to build a versatile platform for prostate cancer imaging and treatment. The structure of these compounds comprises of a lanthanoid metal ion, gadolinium-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (Gd-DOTA)-based binding fragment and, connected to it by a flexible linker, bicalutamide-derived nonsteroidal antiandrogen moiety. A representative gadolinium complex 15 was evaluated as a magnetic resonance imaging (MRI) agent in C57/bl6 male mouse bearing orthotopic TRAMP C2 prostate tumor.

Original languageEnglish
Pages (from-to)6316-6325
Number of pages10
JournalJournal of Medicinal Chemistry
Volume53
Issue number17
DOIs
StatePublished - 9 Sep 2010

Fingerprint

Dive into the research topics of 'Toward development of targeted nonsteroidal antiandrogen-1,4,7,10- tetraazacyclododecane-1,4,7,10-tetraacetic acid-gadolinium complex for prostate cancer diagnostics'. Together they form a unique fingerprint.

Cite this