摘要(英) |
Inspired by the anti-cancer activity of 2-imino-1,2-dihydro-dipyrido[1,2-a:2′,3′-d] pyrimidin-5-one (IP) from in-house library, we synthesized a series of 2-imino-1,2-dihydro- dipyrido[1,2-a:2′,3′-d]pyrimidin-5-one (IP) containing compounds, GX002, GX003, GX004, GX006, GX007, GX008, with modifications of its functional groups. Next, we conducted biological study to test their cytotoxicity against breast cancer cells and evaluate the in vivo efficacy of GX006. Some of the GX compounds had good cytotoxicity to MDA-MB-231 cells, which are triple-negative breast cancer cells. Among of them, the IC50 value of cytotoxicity of the best one can reach around 0.5 to 1 μM. Furthermore, we chose the one, GX006, to the further animal study. The result showed that it can reduce the tumor growth significantly. In summary, this series of 2-imino-1,2-dihydro-dipyrido[1,2-a:2′,3′-d]pyrimidin -5-one containing compounds still have potential to develop into different candidates and study their inhibitory effect toward cancer cells. |
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