• Title/Summary/Keyword: DNA cleaving agents

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Synthesis of 1-(2-Naphthoyl) Benzotriazoles as Photoactivated DNA Cleaving Agents

  • Yang, Jae-Wook;Wender, Paul-A.
    • Archives of Pharmacal Research
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    • v.20 no.2
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    • pp.197-199
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    • 1997
  • In conclusion, benzotriazole analogs prepared in this research showed strong possibility to be photochemically activated DNA cleaving agents. Electrophilic groups such as haloacetoxy groups on the alkyl chain of benzotriazole analogs promote the DNA cleaving ability. Synthesis of 1-(2-Naphthoyl) Benzotriazoles.

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Photocleavage of DNA by 4'-Bromoacetophenone Analogs

  • Jeon, Ra-Ok;Pual A.Wender
    • Archives of Pharmacal Research
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    • v.24 no.1
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    • pp.39-43
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    • 2001
  • 4'-Bromoacetophenone analogs, which are able to generate monophenyl radicals capable of hydrogen atom abstraction, were investigated as possible photoinducible DNA cleaving agents. The potential of 4'-Bromoacetophenone as a possible new DNA cleaver is explored. Pyrrolecarboxatmid conjugated 4'-Bromoacetophenone, in particular, DNA cleaving activity and sequence-selectivity on the contiguous AT base pair sites.

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Photocleavage of DNA by 4′-Bromoacetophenone- Pyrrole Carboxamides

  • Jeon, Raok
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2001.11a
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    • pp.79-79
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    • 2001
  • Genotoxic chemotherapeutics are irreversible DNA targeting agents, which can act as anticancer and antiviral drugs. Natural antibacterial and anticancer enediynes function through the formation of free radicals formed by Bergman-type cycloaromatization and being capable of cleavage of DNA strand. They have been focused primarily on the design and syntheses of simple enediyne structures, which can be mimic their mechanistic feature. Recently. I have been reported the possible application of 4'-bromoacetophenone as a simple photoactivatable DNA cleaving agent, which could be readily prepared and exhibit potent and selective DNA cleaving activity. Herein, we further investigated the activity of 4'-bromoacetophenone-pyrrolecarboxamides, which consist of both DNA cleaving element and recognition unit under various conditions in order to get more understanding of the mechanism of the action and find a broad spectrum of application.

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Effect of Interaction between Protocatechualdehyde Produced from Streptomyces lincolnensis M-20 and Copper Ions on Antioxidant and Pro-oxidant Activities (Streptomyces lincolnensis M-20 균주에서 생산된 Protocatechualdehyde와 구리 이온의 상호 작용이 항 산화 및 산화 촉진 활성에 미치는 영향)

  • Kim, Kyoung-Ja;Lee, Jae-Hun;Yang, Yong-Joon
    • Korean Journal of Microbiology
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    • v.50 no.1
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    • pp.22-26
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    • 2014
  • Protocatechualdehyde (PA) is phenolic compound having antioxidative and antitumor activities. PA was purified from supernatant of Streptomyces lincolnensis M-20. In the presence of copper ion, PA acted as pro-oxidant. The antioxidant activity was assessed with the 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay, and the pro-oxidant effect of PA on DNA damage as pBR322 plasmid DNA-cleaving agents in the presence of Cu(II) ions was investigated. The involvement of reactive oxygen species (ROS) in the DNA damage was confirmed by the inhibition of the DNA breakage by using glutathione (GSH), specific scavenger of ROS. When the increase in ROS reaches a certain level (the toxic threshold), it may trigger cell death. The formation of the PA/Cu(II) chelate complex was confirmed by reaction with ethylenediamine-tetraacetic acid (EDTA), a well-known chelating agent for metal ions, by using UV/Vis spectroscopic analysis.