Synthesis and biological evaluation of dimeric cinnamaldehydes as potent antitumor agents = 시남알데하이드유도체의 합성 및 항암활성 기전 규명

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Title
Synthesis and biological evaluation of dimeric cinnamaldehydes as potent antitumor agents = 시남알데하이드유도체의 합성 및 항암활성 기전 규명
Author(s)
Dae Seop Shin; J H Kim; Su-Kyung Lee; Dong Cho HanKwang Hee Son; Hwan Mook Kim; H G Cheon; K R Kim; N D Sung; S J Lee; S K Kang; Byoung-Mog Kwon
Bibliographic Citation
Bioorganic & Medicinal Chemistry, vol. 14, no. 8, pp. 2498-2506
Publication Year
2006
Abstract
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 μM. 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 G 2/M transition and S phase progression.
Keyword
apoptosisCdc25B phosphatasecell cyclecinnamaldehydedimeric cinnamaldehyde
ISSN
0968-0896
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmc.2005.11.028
Type
Article
Appears in Collections:
Division of Biomedical Research > Personalized Genomic Medicine Research Center > 1. Journal Articles
Division of Biomedical Research > Microbiome Convergence Research Center > 1. Journal Articles
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