Περίληψη:
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.
Συγγραφείς:
Tzanopoulou, Stamatia
Sagnou, Marina
Paravatou-Petsotas, Maria
and Gourni, Eleni
Loudos, George
Xanthopoulos, Stavros and
Lafkas, Daniel
Kiaris, Hippokratis
Varvarigou, Alexandra and
Pirmettis, Ioannis C.
Papadopoulos, Minas
Pelecanou, Maria
