1492924-32-9Relevant academic research and scientific papers
Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents
Liao, Shengrong,Qin, Xiaochu,Li, Ding,Tu, Zhengchao,Li, Jinsheng,Zhou, Xuefeng,Wang, Junfeng,Yang, Bin,Lin, Xiuping,Liu, Juan,Yang, Xianwen,Liu, Yonghong
, p. 236 - 244 (2014/07/08)
Non-protected 2,5-diketopiperazine derivatives have poor solubility thus with negative impact on their bioavailability. In the present study, twenty-one novel soluble mono-protected, and three non-protected 2,5-diketopiperazine derivatives were designed and synthesized. Their anticancer activity to ten cell lines were evaluated by using CCK8 assay, and the results showed that about half of the mono-protected derivatives had broad-spectrum anticancer activity. Among allyl-protected derivatives, compound 4m had strong activity to all the cell lines (IC50 = 0.5-4.5 μM), especially to the cancer cell lines U937 (IC50 = 0.5 μM) and K562 (IC50 = 0.9 μM). Compound 4m could become a lead compound for further development for anticancer agents.
