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

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

  • Eur J Med Chem. 2014 Aug 18:83:236-44. doi: 10.1016/j.ejmech.2014.06.030.
Shengrong Liao 1,  Xiaochu Qin 2,  Ding Li 3,  Zhengchao Tu 2,  Jinsheng Li 1,  Xuefeng Zhou 1,  Junfeng Wang 1,  Bin Yang 1,  Xiuping Lin 1,  Juan Liu 1,  Xianwen Yang 1,  Yonghong Liu 4
Affiliations

Affiliations

  • 1 CAS Key Laboratory of Tropical Marine Bio-resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, PR China.
  • 2 Laboratory of Molecular Engineering and Laboratory of Natural Product Synthesis, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, PR China.
  • 3 School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou 510006, PR China.
  • 4 CAS Key Laboratory of Tropical Marine Bio-resources and Ecology/Guangdong Key Laboratory of Marine Materia Medica/RNAM Center for Marine Microbiology, South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, PR China. Electronic address: yonghongliu@scsio.ac.cn.
PMID: 24960627 DOI: 10.1016/j.ejmech.2014.06.030
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-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.

Keywords

2,5-Diketopiperazine derivative; Anticancer agent; Protective group; Solubility.

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