Structure-activity relationships for G2 checkpoint inhibition by caffeine analogs.

  • Authors:
    • X Jiang
    • L Y Lim
    • J W Daly
    • A H Li
    • K A Jacobson
    • M Roberge
  • View Affiliations

  • Published online on: May 1, 2000     https://doi.org/10.3892/ijo.16.5.971
  • Pages: 971-979
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Abstract

Caffeine inhibits the G2 checkpoint activated by DNA damage and enhances the toxicity of DNA-damaging agents towards p53-defective cancer cells. The relationship between structure and G2 checkpoint inhibition was determined for 56 caffeine analogs. Replacement of the methyl group at position 3 or 7 resulted in loss of activity, while replacement at position 1 by ethyl or propyl increased activity slightly. 8-Substituted caffeines retained activity, but were relatively insoluble. The structure-activity profile did not resemble those for other known pharmacological activities of caffeine. The active analogs also potentiated the killing of p53-defective cells by ionizing radiation, but none was as effective as caffeine.

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May 2000
Volume 16 Issue 5

Print ISSN: 1019-6439
Online ISSN:1791-2423

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APA
Jiang, X., Lim, L., Daly, J., Li, A., Jacobson, K., & Roberge, M. (2000). Structure-activity relationships for G2 checkpoint inhibition by caffeine analogs.. International Journal of Oncology, 16, 971-979. https://doi.org/10.3892/ijo.16.5.971
MLA
Jiang, X., Lim, L., Daly, J., Li, A., Jacobson, K., Roberge, M."Structure-activity relationships for G2 checkpoint inhibition by caffeine analogs.". International Journal of Oncology 16.5 (2000): 971-979.
Chicago
Jiang, X., Lim, L., Daly, J., Li, A., Jacobson, K., Roberge, M."Structure-activity relationships for G2 checkpoint inhibition by caffeine analogs.". International Journal of Oncology 16, no. 5 (2000): 971-979. https://doi.org/10.3892/ijo.16.5.971