Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 83, Issue -, Pages 236-244Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.06.030
Keywords
2,5-Diketopiperazine derivative; Solubility; Anticancer agent; Protective group
Categories
Funding
- National Key Basic Research Program of China (973)'s Project [2010CB833800, 2011CB915503]
- National High Technology Research and Development Program (863 Program) [2012AA092104]
- National Natural Science Foundation of China [31270402, 21172230, 30973679, 41176148, 21002110]
- Guangdong Province-CAS Joint Research Program [2011B090300023, 2012B091100264]
- Guangdong Marine Economic Development and Innovation of Regional Demonstration Project [GD2012-D01-001, GD2012D01-002]
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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 mu M), especially to the cancer cell lines U937 (IC50 = 0.5 mu M) and K562 (IC50 = 0.9 mu M). Compound 4m could become a lead compound for further development for anticancer agents. (C) 2014 Elsevier Masson SAS. All rights reserved.
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