查找使用阿拉丁产品的科研文献

Design and synthesis of novel soluble 2,5-diketopiperazine derivatives as potential anticancer agents

Shengrong Liao,Xiaochu Qin,Ding Li,Zhengchao Tu,Jinsheng Li,Xuefeng Zhou,Junfeng Wang,Bin Yang,Xiuping Lin,Juan Liu,Xianwen Yang,Yonghong Liu

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 (IC 50  = 0.5–4.5 μM), especially to the cancer cell lines U937 (IC 50  = 0.5 μM) and K562 (IC 50  = 0.9 μM). Compound 4m could become a lead compound for further development for anticancer agents .