99mTc-amitrole as a novel selective imaging probe for solid tumor: In silico and preclinical pharmacological study

Lactoperoxidase (LPO) inhibitors are very selective for solid tumor due to their high binding affinity to the LPO enzyme. A computational study was used to select top-ranked LPO inhibitor (alone and in complex with Tc-99m) with high in silico affinity. The novel prepared Tc-99m-amitrole complex demonstrated both in si/ico and in vivo high affinity toward solid tumors. Tc-99m-amitrole was radio-synthesized with a high radiochemical yield (89.7 +/- 3.25). It showed in vitro stability for up to 6 h. Its preclinical evaluation in solid tumor-bearing mice showed high retention and biological accumulation in solid tumor cells with a high Target/Non-Target (TINT) ratio equal to 4.9 at 60 min post-injection. The data described previously could recommend Tc-99m-amitrole as potential targeting scintigraphic probe for solid tumor imaging. (C) 2015 Elsevier B.V. All rights reserved.