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Binding of Carboline Derivatives to Calf Thymus DNA─Determination of Binding Mode and Binding Strength

Ming Yang, Kui Wang, Chuan-Bing Zang, Bao-Huai Wang, You-MinZhang   

  1. 1. National Research haboratories of Natural and Biomimetic Drugs, Beijing Medical University, Beijing 100083;
    2. Institute of Physical Chemistry, Peking University, Beijing 100871
  • Received:1992-05-09 Revised:1993-10-08 Online:1994-06-15 Published:1994-06-15

Abstract: The relationship between anticancer activity of six carboline derivatives (CB1-6)and their binding mode and binding strength with DNA was studied. Binding mode was established by study of structural changes in DNA helix, which involved assessment of changes in the viscosity, 31P NMR and CD spectra of DNA as well as hypochromism in UV-Vis determination and 1H NMR spectra of the aromatic protons of CB1-6 by titration with DNA. Binding strength was evaluated by spectroscopic and microcalorimetric measurements. The results indicate that the binding depends strongly on the ring automaticity and the substituent groups, which accords well with the findings in bioactivity tests.

Key words: DNA, Carboline, Binding mode, Binding strength

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