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In Vitro Imaging and Human Serum Albumin Responsive Dimeric Lanthanide DO3A Complex
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文摘
Two series of dimeric DO3A (1,4,7,10-tetraazacyclodecane-1,4,7-triacetate) lanthanide complexes (LnL1鈥揕nL2, Ln = Eu, Gd, and Tb) have been synthesized with two different bridged chromophores. The X-ray structures of dimeric LnL1 (Ln = Gd and Tb) complexes show that each metal ion has nine coordination numbers with eight directly bound donor atoms of the ligand and one oxygen donor from the water molecule. Photophysical measurements indicate that the bridged antenna in LnL2 gives a higher efficiency than that of LnL1 and is responsive to the protein Human Serum Albumin (HSA), giving an f鈥揻 luminescence signal enhancement with a binding constant log K = 4.84. In vitro imaging of EuL1 and EuL2 in HeLa cells has been recorded, and EuL2 has demonstrated a higher rate of cellular uptake and low cytotoxicity (IC50 = 3 mM).

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