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.
Satpati
Drishty
D
Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Mumbai 400085, India.
Korde
Aruna
A
Venkatesh
Meera
M
Banerjee
Sharmila
S
D000818:Animals; D018906:Antineoplastic Agents, Alkylating / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D045744:Cell Line, Tumor; D002699:Chlorambucil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D005354:Fibrosarcoma / Q000000981:diagnostic imaging / Q000378:metabolism; D006801:Humans; D051379:Mice; D009368:Neoplasm Transplantation; D015609:Organotechnetium Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D011869:Radioligand Assay; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000493:pharmacokinetics*; D014018:Tissue Distribution
D018906:Antineoplastic Agents, Alkylating; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D002699:Chlorambucil