Herein we have identified selenadiazole derivatives as effective and safe theranostic agents for simultaneous cancer chemo-/radiotherapy.

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This study demonstrates the construction of a cancer-targeted nanosystem as payload of iron complexes to reverse cancer multidrug resistance.

Hyperglycemia is an important factor for chemoresistance of breast cancer patients with diabetes. In the present study, a novel selenadiazole derivative has been evaluated and found to be able to antagonize the doxorubicin (DOX) resistance of MCF-7 cells under simulated diabetes conditions. Hyperglycemia promotes the proliferation, invasion and migration of MCF-7 cells through activation of ERK and AKT pathways, which could be inhibited by the synthetic selenadiazole derivative. The antitumor effects of the selenadiazole derivative were attributed to its ability to activate AMPK pathways. Furthermore, the high lipophilicity (log P = 1.9) of the synthetic selenadiazole derivative facilitated its uptake by cancer cells and subsequently potentiated the cellular uptake of DOX, leading to a strong enhancment of the antiproliferative activity of DOX on MCF-7 cells by induction of apoptosis. The apoptosis was initiated by the ROS overproduction induced by the cooperation of the selenadiazole derivative and DOX. The excessive ROS then caused damage to DNA, which upregulated the expression of proapoptosis Bcl-2 family proteins and led to fragmentation of mitochondria, which finally caused apoptosis of the cancer cells. Taken together, this study provides a rational strategy for using selenadiazole derivatives to overcome hyperglycemia-induced drug resistance in breast cancer by activation of AMPK-mediated pathways.

A simple, efficient, inexpensive one-pot method for the benzo[d][1,3]selenazole derivatives synthesized from 2-bromoaniline was developed by using cheap carbon-supported copper as catalyst at room temperature. The reaction provides an efficient protocol to a series of benzo[d][1,3]selenazole derivatives in good to high yields, and benefits of readily available catalyst and synthesis of high efficiency.