Synthesis, characterization, and biological evaluation of M(I)(CO)3(NNO) complexes (M = Re, 99mTc) conjugated to 2-(4-aminophenyl)benzothiazole as potential breast cancer radiopharmaceuticals.

Abstract

The synthesis and biological evaluation of new M(I)(CO)3(NNO) (M = Re, 99mTc) complexes attached to the antitumor agent 2-(4-aminophenyl)benzothiazole are reported. The fluorescent rhenium complex enters MCF-7 breast cancer cells but does not enter normal HFFF-2 and MRC-5 cells. The analogous radioactive 99mTc complex produces fast blood and soft tissue clearance when administered to healthy mice. These complexes are promising candidates for developing radiopharmaceuticals for imaging (99mTc) and targeted radiotherapy (186Re, 188Re) of breast cancer.

• Authors: Stamatia Tzanopoulou, Ioannis C Pirmettis, George Patsis, Maria Paravatou-Petsotas, Evangelia Livaniou, Minas Papadopoulos, Maria Pelecanou
• Journal: Journal of medicinal chemistry (J Med Chem) Vol. 49 Issue 18 Pg. 5408-10 (Sep 07 2006) ISSN: 0022-2623 [Print] United States
• PMID: 16942013 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 2-(4-aminophenyl)benzothiazole
• Antineoplastic Agents
• Benzothiazoles
• Organometallic Compounds
• Radiopharmaceuticals
• Thiazoles
• Rhenium
• Technetium

Topics

• Animals
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Benzothiazoles
• Breast Neoplasms (diagnostic imaging, metabolism)
• Cell Line
• Cell Line, Tumor
• Female
• Fibroblasts (metabolism)
• Humans
• Mice
• Organometallic Compounds (chemical synthesis, chemistry, pharmacology)
• Radiopharmaceuticals (chemical synthesis, chemistry, pharmacology)
• Rhenium
• Structure-Activity Relationship
• Technetium
• Thiazoles (chemistry)
• Tomography, Emission-Computed, Single-Photon