@article{3146305, title = "Evaluation of Re and Tc-99m Complexes of 2-(4 `-Aminophenyl)benzothiazole as Potential Breast Cancer Radiopharmaceuticals", author = "Tzanopoulou, Stamatia and Sagnou, Marina and Paravatou-Petsotas, Maria and and Gourni, Eleni and Loudos, George and Xanthopoulos, Stavros and and Lafkas, Daniel and Kiaris, Hippokratis and Varvarigou, Alexandra and and Pirmettis, Ioannis C. and Papadopoulos, Minas and Pelecanou, Maria", journal = "Journal of Medicinal Chemistry", year = "2010", volume = "53", number = "12", pages = "4633-4641", publisher = "AMER CHEMICAL SOC", issn = "0022-2623, 1520-4804", doi = "10.1021/jm1001293", abstract = "The synthesis of M(I)(CO)(3)(NNO) (M = Re, Tc-99m) complexes conjugated to the antitumor agent 2-(4’-aminophenyl)benzothiazole and to its 6-methyl derivative, as well as their in vitro and in vivo biological evaluation as breast cancer radiopharmaceuticals, is reported. The Re complexes displayed under the fluorescence microscope clear uptake by the sensitive to the 2-(4’-aminophenyl)benzothiazole pharmacophore breast cancer cell lines MCF-7 and T47D, while uptake by less sensitive lines and by normal fibroblasts was much weaker. In accordance, uptake of the corresponding radioactive Tc-99m complexes was clearly higher in the breast cancer cell lines MCF-7 and MDA-231 compared to normal fibroblasts. Biodistribution of the Tc-99m complexes in SCID mice bearing MCF-7 xenografts showed appreciable tumor uptake. A tumor/muscle ratio of 2.2 was measured for the complex conjugated to 2-(4’-aminophenyl)benzothiazole that led to successful tumor imaging. The results render the 2-(4’-aminophenyl)benzothiazole complexes potential candidates for imaging (Tc-99m) and targeted radiotherapy (Re-188) of breast cancer." }