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| Synthesis and Cytotoxic Activities of 2,5-Diketopiperazine Derivatives by One-pot Method |
| LI Jin-sheng1,2, LIAO Sheng-rong1, TANG Yong1,2, LIU Yong-hong1 |
| 1. South China Sea Institute of Oceanology, Chinese Academy of Sciences, Guangzhou 510301, China; 2. University of Chinese Academy of Sciences, Beijing 100049, China |
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Abstract Ten 2,5-diketopiperazine derivatives(4a~4j, 4c, 4f and 4i were novel compounds) in yield of 54.2～75.7％ were synthesized by Aldol reaction of N,N-diacetyl-2,5-diketopiperazine, arylaldehyde and RX by onepot method, using DMF as the solvent and Cs2CO3 as the alkali. The structures were confirmed by 1H NMR， 13C NMR and ESI-MS. Preliminary biological activities tests indicated that (Z)-1-acetyl-4-allyl-3-(naphthalen-1-ylmethylene)piperazine-2,5-dione(4c) exhibited better cytotoxic activities against U937, Hela and Du145 cell lines.
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Received: 16 January 2015
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2015, Vol. 23 
