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

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 radioa...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2006-09, Vol.49 (18), p.5408-5410
Main Authors: Tzanopoulou, Stamatia, Pirmettis, Ioannis C, Patsis, George, Paravatou-Petsotas, Maria, Livaniou, Evangelia, Papadopoulos, Minas, Pelecanou, Maria
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Benzothiazoles
Biological and medical sciences
Breast Neoplasms - diagnostic imaging
Breast Neoplasms - metabolism
Cell Line
Cell Line, Tumor
Contrast media. Radiopharmaceuticals
Female
Fibroblasts - metabolism
Humans
Medical sciences
Mice
Organometallic Compounds - chemical synthesis
Organometallic Compounds - chemistry
Organometallic Compounds - pharmacology
Pharmacology. Drug treatments
Radiopharmaceuticals - chemical synthesis
Radiopharmaceuticals - chemistry
Radiopharmaceuticals - pharmacology
Rhenium
Structure-Activity Relationship
Technetium
Thiazoles - chemistry
Tomography, Emission-Computed, Single-Photon
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm0606387