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

…, Z Tu, J Li, X Zhou, J Wang, B Yang, X Lin, J Liu…

Index: Liao, Shengrong; Qin, Xiaochu; Li, Ding; Tu, Zhengchao; Li, Jinsheng; Zhou, Xuefeng; Wang, Junfeng; Yang, Bin; Lin, Xiuping; Liu, Juan; Yang, Xianwen; Liu, Yonghong European Journal of Medicinal Chemistry, 2014 , vol. 83, p. 236 - 244

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Citation Number: 9

Abstract

Abstract 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- ...