Preparation and bioevaluation of a 99mTc-labeled chlorambucil analog as a tumor targeting agent.

Chlorambucil belongs to a group of nitrogen mustards which are used for the treatment of variety of cancers. Hence, a chlorambucil derivative has been radiolabeled with [(99m)Tc(CO)(3)(H(2)O)(3)](+) core and its efficacy as a tumor targeting agent has been evaluated. Radiochemical yield of the complex was >98% as observed by HPLC. The in vitro studies in MCF-7 breast cancer cells showed about 30% inhibition of the radiolabeled complex in presence of the cold chlorambucil derivative. Biodistribution studies in Swiss mice bearing fibrosarcoma tumor showed an uptake of 3.2+/-0.3%ID/g at 3h.p.i.