Exploring the prospective of Tc-99m-labeled DNA intercalator in tumor imaging: Studies with Tc-99m-acridine

作者：Ghosh, Subhajit; Suman, Shishu K.; Sarma, Haladhar D.; Das, Tapas^*

来源：Polyhedron, 2021, 204: 115276.

DOI：10.1016/j.poly.2021.115276

• Radiolabeled DNA intercalators
• Acridine
• Tc-99m
• [(TcN)-Tc-99m](2+)core
• Tc-99m-acridine

Acridine or its suitable derivatives are expected to preferentially accumulate in the tumors owing to their DNA intercalation property, as tumors are invariably associated with enhanced DNA replication. Therefore, Tc-99m-labeled acridine is likely to have potential in diagnosis of tumorous lesions. To explore this possibility, 9-aminoacridine was converted to its corresponding dithiocarbamate derivative and subsequently radiolabeled with Tc-99m using pre-formed [(TcN)-Tc-99m](2+) intermediate. In-vitro cell studies in Raji cell line showed encouraging cell uptake, while biodistribution study in tumor bearing Swiss mice revealed significant accumulation of activity in tumor and retention therein. Present study, although preliminary, indicated the potential of (TcN)-Tc-99m-acridine complex for imaging of tumorous lesions.