Photochemical Activation of Enediyne Warheads: A Potential Tool for Targeted Antitumor Therapy

Mol Pharm. 2018 Mar 5;15(3):768-797. doi: 10.1021/acs.molpharmaceut.7b00911. Epub 2018 Feb 1.

Abstract

Spatial and temporal control over DNA cleavage by photoactivated enediynes can be complemented by additional factors such as the release of internal strain, chelation, pH changes, intramolecular H-bonds, and substituent effects. This review presents design and reactivity of photoactivated enediynes/enynes and analyses the chemical, biological, and photophysical challenges in their applications.

Keywords: Bergman cyclization; DNA cleavage; DNA damage; apoptosis; diradicals; enediynes; photoactivation.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Antibiotics, Antineoplastic / chemistry
  • Antibiotics, Antineoplastic / pharmacology*
  • Antibiotics, Antineoplastic / radiation effects
  • Antibiotics, Antineoplastic / therapeutic use
  • Cyclization / radiation effects
  • DNA Damage / drug effects
  • DNA Damage / radiation effects
  • DNA, Neoplasm / chemistry
  • DNA, Neoplasm / drug effects*
  • DNA, Neoplasm / radiation effects
  • Enediynes / chemistry
  • Enediynes / pharmacology*
  • Enediynes / radiation effects
  • Enediynes / therapeutic use
  • Humans
  • Light
  • Lysine / chemistry
  • Molecular Structure
  • Molecular Targeted Therapy / methods
  • Neoplasms / drug therapy*
  • Neoplasms / genetics
  • Photochemotherapy / methods*

Substances

  • Antibiotics, Antineoplastic
  • DNA, Neoplasm
  • Enediynes
  • Lysine