Leukemia is a kind of blood cancer, begins in the bone marrow and results in abnormal blood cells. It severely affects the patients. The need for more drugs with fewer side effects is increasing. Researchers synthesize a series of compounds to examine their biological activities. As a result, BTR-1 becomes most potent among these products.

BTR-1 is a rhodanine derivative. The latter proves to be a promising compound. It possesses effective biological activity, such as anticonvulsant, antibacterial, antiviral, and antidiabetic effect. However, their anti-cancer activity is unclear. Thus, researchers carry out a couple of steps to examine the potency of the compound.

Firstly, in cellular assays, BTR-1 causes cytotoxicity to leukemic cell line, with an IC50 of <10 μM. In T-cell leukemic cell lines, BTR-1 (10, 50, 100, or 250 μM) dose-dependently induces cytotoxicity in cells. The induction is also time-dependent. Besides, in MTT assay, BTR-1 affects the proliferation of T-cell leukemic cells at as low as 10 μM. In addition, in LDH release assay, BTR-1 (10, 50, 100, or 250 μM) increases LDH release in a dose- and time-dependent manner.

Then, BTR-1 continues to further study. It may have effect on S phase of cell cycle, and induces DNA fragmentation. BTR-1 results in breakage in CEM cells at 10 μM. Furthermore, BTR-1 (20 μM) leads to ROS production in CEM cells.

In a word, BTR-1 potently inhibits cell growth. It induces S phase arrest, affects DNA replication. BTR-1 increases ROS production and DNA strand breaks, activates apoptosis for induction of cell death. BTR-1 needs further study to exhibit more potential in cancer research. Hope it plays a vital role in cancer treatment.

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6297-301.