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Title 

Synthesis and biological evaluation of dimeric cinnamaldehydes as potent antitumor agents

 

시남알데하이드유도체의 합성 및 항암활성 기전 규명

Authors 

Dae Seop ShinJ H KimSu-Kyung LeeDong Cho HanKwang Hee SonHwan Mook KimH G CheonK R KimN D SungS J LeeS K KangByoung-Mog Kwon

Publisher 

Elsevier

Issue Date 

2006

Citation 

Bioorganic & Medicinal Chemistry, vol. 14, no. 8, pp. 2498-2506

Keywords 

apoptosisCdc25B phosphatasecell cyclecinnamaldehydedimeric cinnamaldehydedrug synthesisevaluationantineoplastic agents

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.

ISSN 

0968-0896

Link 

http://dx.doi.org/10.1016/j.bmc.2005.11.028

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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