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Designed enediynes - a new class of DNA-cleaving molecules with potent and selective anticancer activity

Academic Article
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Overview

authors

  • Nicolaou, K.C.
  • Dai, W. M.
  • Tsay, S. C.
  • Estevez, V. A.
  • Wrasidlo, W.

publication date

  • 1992

journal

  • Science  Journal

abstract

  • The rational design and biological actions of a new class of DNA-cleaving molecules with potent and selective anticancer activity are reported. These relatively simple enediyne-type compounds were designed from basic chemical principles to mimic the actions of the rather complex naturally occurring enediyne anticancer antibiotics, particularly dynemicin A. Equipped with locking and triggering devices, these compounds damage DNA in vitro and in vivo on activation by chemical or biological means. Their damaging effects are manifested in potent anticancer activity with remarkable selectivities. Their mechanism of action involves intracellular unlocking and triggering of a Bergman reaction, leading to highly reactive benzenoid diradicals that cause severe DNA damage. The results of these studies demonstrate the potential of these de novo designed molecules as biotechnology tools and anticancer agents.

subject areas

  • Antibiotics, Antineoplastic
  • Antineoplastic Agents
  • Cell Line
  • Cell Survival
  • DNA Damage
  • Dose-Response Relationship, Drug
  • Drug Design
  • Female
  • Humans
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Structure-Activity Relationship
  • Tumor Cells, Cultured
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Identity

International Standard Serial Number (ISSN)

  • 0036-8075

Digital Object Identifier (DOI)

  • 10.1126/science.256.5060.1172

PubMed ID

  • 1589797
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Additional Document Info

start page

  • 1172

end page

  • 1178

volume

  • 256

issue

  • 5060

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