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Shin DS, Kim JH, Lee SK, Han DC, Son KH, Kim HM, Cheon HG, Kim KR, Sung ND, Lee SJ, Kang SK, Kwon BM: Synthesis and biological evaluation of dimeric cinnamaldehydes as potent antitumor agents. Bioorg Med Chem. 2006 Apr 15;14(8):2498-506. Epub 2005 Dec 15.
It has been reported that 2-hydroxycinnamaldehyde and 2-benzoyl-oxycinnamaldehyde inhibited the activity of farnesyl protein transferase, angiogenesis, cell-cell adhesion, and tumor growth in vivo model. In order to improve its anti-tumor activity, dimeric cinnamaldehydes have been synthesized based on 2-hydroxycinnamaldehyde. The synthesized compounds strongly inhibited the growth of human colon tumor cells with GI50 values of 0.6-10 microM. Especially, 2-piperazine derivative blocked in vivo growth of human colon tumor xenograft in nude mice at 10 mg/kg. It was found that their anti-tumor effects induce apoptosis and cell cycle arrest at G2/M phase by the compounds. It was confirmed by detection of apoptosis markers such as activated caspase-3 and cleaved PARP, and cell cycle analysis. The dimeric compounds also inhibited Cdc25B phosphatase which is essential for preinitiating G2/M transition and S phase progression. |
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