Synthesis, cytotoxicity and Tc-MIBI tumor cell uptake evaluation of 2-phenylbenzothiazole tagged triazole derivatives.

The extensive utilization of 2-phenylbenzothiazole due to their wide array of biological activities, particularly in cancer therapy, has caused great attention to explore more potent derivatives. We report the synthesis of 2-phenylbenzothiazole tagged 1,2,3-triaozle through Cu(I)-catalyzed cycloaddition of alkyne side chain with aryl-substituted azides. The experiments, using MTT and 99mTc-MIBI cell uptake methods, demonstrated the remarkable anticancer activity of these compounds against A549, SKOV3 and MCF7 cell lines. Compounds , and possessed high cytotoxic activity as compared with doxorubicin. Compound has a similar inhibitory effect on the proliferation of breast cancer cells as doxorubicin. study indicated that compound would be a good lead for the development of new potent anticancer agents.