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Related Concept Videos

2° Amines to N-Nitrosamines: Reaction with NaNO201:20

2° Amines to N-Nitrosamines: Reaction with NaNO2

Secondary amines react with nitrous acid to form N-nitrosamines, as depicted in Figure 1. Nitrous acid, a weak and unstable acid, is formed in situ from an aqueous solution of sodium nitrite and strong acids, such as hydrochloric acid or sulfuric acid, in cold conditions. In the presence of an acid, the nitrous acid gets protonated. The subsequent loss of water results in the formation of the electrophile known as nitrosonium ion.
Aryldiazonium Salts to Azo Dyes: Diazo Coupling01:11

Aryldiazonium Salts to Azo Dyes: Diazo Coupling

The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the para position.

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Formation of Covalent DNA Adducts by Enzymatically Activated Carcinogens and Drugs In Vitro and Their Determination by 32P-postlabeling
09:33

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Radiosensitization with a 3-nitrotriazole (ak-2123).

M Imamura1, M Edgren, T Murata

  • 1KAROLINSKA INST,DEPT MED RADIAT PHYS,DIV TUMOR BIOL,STOCKHOLM,SWEDEN. KANSAI MED UNIV,DEPT INTERNAL MED 3,OSAKA,JAPAN.

International Journal of Oncology
|May 11, 2011
PubMed
Summary
This summary is machine-generated.

AK-2123 enhances radiation therapy by increasing DNA damage and cell death in V79 cells. This radiosensitizing effect is concentration-dependent, with no short-term cytotoxicity observed.

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Area of Science:

  • Radiobiology
  • Cellular and Molecular Biology

Background:

  • Understanding the mechanisms of radiosensitizers is crucial for improving cancer therapy.
  • AK-2123 is a novel compound with potential radiosensitizing properties.

Purpose of the Study:

  • To elucidate the mechanism of action of AK-2123 as a radiosensitizer.
  • To evaluate the dose-response relationship and efficacy of AK-2123 in V79 cells.

Main Methods:

  • V79 cells were exposed to varying X-ray doses after treatment with AK-2123.
  • End-points assessed included DNA breaks, micronuclei formation, and clonogenic survival.
  • Drug concentrations ranged from 0.001 to 50 mmol dm(-3) to determine K-values and maximum enhancement ratios.

Main Results:

  • AK-2123 demonstrated radiosensitizing effects, with sensitization factors of 1.8 (DNA breaks), 1.1 (micronuclei), and 1.4 (survival) at 0.1 mmol dm(-3).
  • K-values for maximum sensitization were 40 μmol dm(-3) (DNA breaks), 1200 μmol dm(-3) (micronuclei), and 2000 μmol dm(-3) (survival).
  • Maximum sensitizer enhancement ratios reached 2.4 (DNA breaks), 2.3 (micronuclei), and 2.4 (survival).
  • Cytotoxicity was observed at longer exposure times and higher concentrations under both aerobic and hypoxic conditions.
  • Post-irradiation enhancement of sensitivity was noted when the drug remained in the medium for 24 hours.

Conclusions:

  • AK-2123 acts as a potent radiosensitizer, enhancing radiation-induced DNA damage and cell death.
  • The compound exhibits concentration- and time-dependent cytotoxicity, with significant radiosensitizing effects observed even after irradiation.