TY - JOUR
TI - Evaluation of Re and Tc-99m Complexes of 2-(4
`-Aminophenyl)benzothiazole as Potential Breast Cancer
Radiopharmaceuticals
AU - Tzanopoulou, Stamatia
AU - Sagnou, Marina
AU - Paravatou-Petsotas, Maria
AU - and Gourni, Eleni
AU - Loudos, George
AU - Xanthopoulos, Stavros and
AU - Lafkas, Daniel
AU - Kiaris, Hippokratis
AU - Varvarigou, Alexandra and
AU - Pirmettis, Ioannis C.
AU - Papadopoulos, Minas
AU - Pelecanou, Maria
JO - Journal of Medicinal Chemistry
PY - 2010
VL - 53
TODO - 12
SP - 4633-4641
PB - AMER CHEMICAL SOC
SN - 0022-2623, 1520-4804
TODO - 10.1021/jm1001293
TODO - null
TODO - 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.
ER -