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Updated: Oct 10, 2026

Formation of Covalent DNA Adducts by Enzymatically Activated Carcinogens and Drugs In Vitro and Their Determination by 32P-postlabeling
Published on: March 20, 2018
Functionalized and [a]-anellated carbazoles as potential B-DNA ligands: experimental studies of DNA binding and
U Pindur1, A Marotto, E Schulze
1Institut für Pharmazie, Fachbereich Chemie und Pharmazie, Johannes-Gutenberg-Universität, Mainz, Germany. pindur@mail.uni-mainz.de
Abstract:
Three synthetically available carbazole derivatives 3-5 were investigated for DNA binding (ethidium bromide displacement assay, DNA unwinding assay), for inhibition of topoisomerase I and for cell cytotoxicity (antitumour cell lines). In addition molecular modeling studies of DNA complexes were performed by semiempirical quantum chemistry, force field calculations and molecular dynamics calculations. In summary, combining the results from experiments and molecular modeling, the naphthoquinone anellated carbazole 4 emerges as a promising antitumour active candidate for further drug design studies in carbazole chemistry.
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