Medicinal Chemistry

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

DOI: 10.2174/157340612801216256

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

Page: [727 - 731] Pages: 5

  • * (Excluding Mailing and Handling)

Abstract

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