Bioorganic and Medicinal Chemistry Letters 2012-Dec
Synthesis and biological evaluation of ⁹⁹mTc(CO)₃(His-CB) as a tumor imaging agent.
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The chlorambucil l-histidine conjugate was synthesized and radiolabeled with [(99m)Tc(CO)(3)](+) core to form the (99m)Tc(CO)(3)(His-CB) complex. The radiochemical purity of the complex was over 90%. It had good hydrophilicity and was stable at room temperature. The high initial tumor uptake with certain retention, fast clearance from background, good tumor/non-tumor ratios and satisfactory scintigraphic images highlighted the potential of (99m)Tc(CO)(3)(His-CB) as a tumor imaging agent.