Synthesis and biological evaluation of dimeric cinnamaldehydes as potent antitumor agents. 2006

Dae-Seop Shin, and Jong-Han Kim, and Su-Kyung Lee, and Dong Cho Han, and Kwang-Hee Son, and Hwan-Mook Kim, and Hyae-Gyeong Cheon, and Kwang-Rok Kim, and Nack-Do Sung, and Seung Jae Lee, and Sung Kwon Kang, and Byoung-Mog Kwon
Korea Research Institute of Bioscience and Biotechnology, 52 Uendong Yoosung, Taejeon 305-600, Republic of Korea.

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.

UI MeSH Term Description Entries
D008819 Mice, Nude Mutant mice homozygous for the recessive gene "nude" which fail to develop a thymus. They are useful in tumor studies and studies on immune responses. Athymic Mice,Mice, Athymic,Nude Mice,Mouse, Athymic,Mouse, Nude,Athymic Mouse,Nude Mouse
D008958 Models, Molecular Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures. Molecular Models,Model, Molecular,Molecular Model
D009682 Magnetic Resonance Spectroscopy Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING). In Vivo NMR Spectroscopy,MR Spectroscopy,Magnetic Resonance,NMR Spectroscopy,NMR Spectroscopy, In Vivo,Nuclear Magnetic Resonance,Spectroscopy, Magnetic Resonance,Spectroscopy, NMR,Spectroscopy, Nuclear Magnetic Resonance,Magnetic Resonance Spectroscopies,Magnetic Resonance, Nuclear,NMR Spectroscopies,Resonance Spectroscopy, Magnetic,Resonance, Magnetic,Resonance, Nuclear Magnetic,Spectroscopies, NMR,Spectroscopy, MR
D002455 Cell Division The fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION. M Phase,Cell Division Phase,Cell Divisions,Division Phase, Cell,Division, Cell,Divisions, Cell,M Phases,Phase, Cell Division,Phase, M,Phases, M
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000171 Acrolein Unsaturated three-carbon aldehyde. 2-Propenal,Acraldehyde,Acrylaldehyde,Acrylic Aldehyde,Allyl Aldehyde,Aqualin,Ethylene Aldehyde,2 Propenal,Aldehyde, Acrylic,Aldehyde, Allyl,Aldehyde, Ethylene
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000970 Antineoplastic Agents Substances that inhibit or prevent the proliferation of NEOPLASMS. Anticancer Agent,Antineoplastic,Antineoplastic Agent,Antineoplastic Drug,Antitumor Agent,Antitumor Drug,Cancer Chemotherapy Agent,Cancer Chemotherapy Drug,Anticancer Agents,Antineoplastic Drugs,Antineoplastics,Antitumor Agents,Antitumor Drugs,Cancer Chemotherapy Agents,Cancer Chemotherapy Drugs,Chemotherapeutic Anticancer Agents,Chemotherapeutic Anticancer Drug,Agent, Anticancer,Agent, Antineoplastic,Agent, Antitumor,Agent, Cancer Chemotherapy,Agents, Anticancer,Agents, Antineoplastic,Agents, Antitumor,Agents, Cancer Chemotherapy,Agents, Chemotherapeutic Anticancer,Chemotherapy Agent, Cancer,Chemotherapy Agents, Cancer,Chemotherapy Drug, Cancer,Chemotherapy Drugs, Cancer,Drug, Antineoplastic,Drug, Antitumor,Drug, Cancer Chemotherapy,Drug, Chemotherapeutic Anticancer,Drugs, Antineoplastic,Drugs, Antitumor,Drugs, Cancer Chemotherapy
D045744 Cell Line, Tumor A cell line derived from cultured tumor cells. Tumor Cell Line,Cell Lines, Tumor,Line, Tumor Cell,Lines, Tumor Cell,Tumor Cell Lines
D051379 Mice The common name for the genus Mus. Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus

Related Publications

Dae-Seop Shin, and Jong-Han Kim, and Su-Kyung Lee, and Dong Cho Han, and Kwang-Hee Son, and Hwan-Mook Kim, and Hyae-Gyeong Cheon, and Kwang-Rok Kim, and Nack-Do Sung, and Seung Jae Lee, and Sung Kwon Kang, and Byoung-Mog Kwon
March 2014, Bioorganic & medicinal chemistry letters,
Dae-Seop Shin, and Jong-Han Kim, and Su-Kyung Lee, and Dong Cho Han, and Kwang-Hee Son, and Hwan-Mook Kim, and Hyae-Gyeong Cheon, and Kwang-Rok Kim, and Nack-Do Sung, and Seung Jae Lee, and Sung Kwon Kang, and Byoung-Mog Kwon
July 2005, Bioorganic & medicinal chemistry letters,
Dae-Seop Shin, and Jong-Han Kim, and Su-Kyung Lee, and Dong Cho Han, and Kwang-Hee Son, and Hwan-Mook Kim, and Hyae-Gyeong Cheon, and Kwang-Rok Kim, and Nack-Do Sung, and Seung Jae Lee, and Sung Kwon Kang, and Byoung-Mog Kwon
May 2015, Bioorganic & medicinal chemistry,
Dae-Seop Shin, and Jong-Han Kim, and Su-Kyung Lee, and Dong Cho Han, and Kwang-Hee Son, and Hwan-Mook Kim, and Hyae-Gyeong Cheon, and Kwang-Rok Kim, and Nack-Do Sung, and Seung Jae Lee, and Sung Kwon Kang, and Byoung-Mog Kwon
December 2022, Journal of enzyme inhibition and medicinal chemistry,
Dae-Seop Shin, and Jong-Han Kim, and Su-Kyung Lee, and Dong Cho Han, and Kwang-Hee Son, and Hwan-Mook Kim, and Hyae-Gyeong Cheon, and Kwang-Rok Kim, and Nack-Do Sung, and Seung Jae Lee, and Sung Kwon Kang, and Byoung-Mog Kwon
August 2002, Bioorganic & medicinal chemistry letters,
Dae-Seop Shin, and Jong-Han Kim, and Su-Kyung Lee, and Dong Cho Han, and Kwang-Hee Son, and Hwan-Mook Kim, and Hyae-Gyeong Cheon, and Kwang-Rok Kim, and Nack-Do Sung, and Seung Jae Lee, and Sung Kwon Kang, and Byoung-Mog Kwon
March 2017, Bioorganic & medicinal chemistry,
Dae-Seop Shin, and Jong-Han Kim, and Su-Kyung Lee, and Dong Cho Han, and Kwang-Hee Son, and Hwan-Mook Kim, and Hyae-Gyeong Cheon, and Kwang-Rok Kim, and Nack-Do Sung, and Seung Jae Lee, and Sung Kwon Kang, and Byoung-Mog Kwon
July 2015, Bioorganic & medicinal chemistry,
Dae-Seop Shin, and Jong-Han Kim, and Su-Kyung Lee, and Dong Cho Han, and Kwang-Hee Son, and Hwan-Mook Kim, and Hyae-Gyeong Cheon, and Kwang-Rok Kim, and Nack-Do Sung, and Seung Jae Lee, and Sung Kwon Kang, and Byoung-Mog Kwon
September 2006, Journal of medicinal chemistry,
Dae-Seop Shin, and Jong-Han Kim, and Su-Kyung Lee, and Dong Cho Han, and Kwang-Hee Son, and Hwan-Mook Kim, and Hyae-Gyeong Cheon, and Kwang-Rok Kim, and Nack-Do Sung, and Seung Jae Lee, and Sung Kwon Kang, and Byoung-Mog Kwon
June 2009, Bioorganic & medicinal chemistry,
Dae-Seop Shin, and Jong-Han Kim, and Su-Kyung Lee, and Dong Cho Han, and Kwang-Hee Son, and Hwan-Mook Kim, and Hyae-Gyeong Cheon, and Kwang-Rok Kim, and Nack-Do Sung, and Seung Jae Lee, and Sung Kwon Kang, and Byoung-Mog Kwon
November 2020, Bioorganic chemistry,
Copied contents to your clipboard!