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DNA but not topoisomerases is a target for a cytotoxic benzo[5,6]cyclohepta[b]indol-6-one derivative.

Abstract
The interaction of a newly designed benzocycloheptaindol-6-one derivative with DNA has been investigated by complementary spectroscopic techniques including absorption, circular and linear dichroism. Footprinting measurements were performed to delineate the sequence-selectivity of the drug-DNA interaction and a plasmid relaxation assay was used to study the effects of the drug on human DNA topoisomerases I and II. The results clearly indicated that the test compound behaves as a typical DNA intercalating agent but does not stimulate DNA cleavage by topoisomerases. At the cellular level, the cytometry measurements showed that the drug provoked a marked accumulation of HL60 human leukemia cells in the G2/M phase of the cell cycle. DNA is thus identified as a valid target for this new series of drugs particularly toxic to human (HL60) and murine (P388) leukemia cells.
AuthorsJ Benoit, S Routier, J Y Mérour, P Colson, C Houssier, C Bailly
JournalAnticancer research (Anticancer Res) 2000 Sep-Oct Vol. 20 Issue 5A Pg. 3307-14 ISSN: 0250-7005 [Print] Greece
PMID11062758 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antineoplastic Agents
  • Cycloheptanes
  • DNA, Neoplasm
  • DNA Topoisomerases, Type I
  • DNA Topoisomerases, Type II
Topics
  • Animals
  • Antineoplastic Agents (chemistry, pharmacology)
  • Cell Cycle
  • Cycloheptanes (chemistry, pharmacology)
  • DNA Topoisomerases, Type I (metabolism)
  • DNA Topoisomerases, Type II (metabolism)
  • DNA, Neoplasm (drug effects)
  • HL-60 Cells
  • Humans
  • Mice
  • Molecular Conformation

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