Propylene Cross-Bridged Macrocyclic Bifunctional Chelator: A New Design for Facile Bioconjugation and Robust 64Cu Complex Stability
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- 作者：Darpan N. Pandya ; Nikunj Bhatt ; Gwang Il An ; Yeong Su Ha ; Nisarg Soni ; Hochun Lee ; Yong Jin Lee ; Jung Young Kim ; Woonghee Lee ; Heesu Ahn ; Jeongsoo Yoo
- 刊名：Journal of Medicinal Chemistry
- 出版年：2014
- 出版时间：September 11, 2014
- 年：2014
- 卷：57
- 期：17
- 页码：7234-7243
- 全文大小：437K
- ISSN：1520-4804
文摘
The first macrocyclic bifunctional chelator incorporating propylene cross-bridge was efficiently synthesized from cyclam in seven steps. After the introduction of an extra functional group for facile conjugation onto the propylene cross-bridge, the two carboxylic acid pendants could contribute to strong coordination of Cu(II) ions, leading to a robust Cu complex. The cyclic RGD peptide conjugate of PCB-TE2A-NCS was prepared and successfully radiolabeled with 64Cu ion. The radiolabeled peptide conjugate was evaluated in vivo through a biodistribution study and animal PET imaging to demonstrate high tumor uptake with low background.