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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Synthesis and 188Re Radiolabelling of Dendrimer Polyamide Amine (PAMAM) Folic Acid Conjugate

Author(s): Wei Cui, Yuanqing Zhang, Xiaoping Xu and Yu-Mei Shen

Volume 8, Issue 4, 2012

Page: [727 - 731] Pages: 5

DOI: 10.2174/157340612801216256

Price: $65


Folic acid receptors (FR) are usually over expressed in many cancer cells and are considered as potential targeted therapy agent. Generation of five polyamido amine (PAMAM) dendrimer folic acid conjugate was synthesised and radiolabelled with 188Re, furthermore the in vitro/in vivo stability was evaluated accordingly. The labelling yield of the conjugate G5-FA-DTPA-188Re was 67.1 % and its radiochemical purity exceeded 95 %. The conjugate also showed high in vitro stability and potential value for further structure modifications and evaluations.

Keywords: Dendrimer, Folic acid, PAMAM, Radiolabelled, Rhenium, polyamido amine, Rhenium-188, micro-SPECT, in vitro, fluorescein

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