Action of a novel pyrrolo[1,2-c][1.3]benzodiazepine on the viability of Jurkat and neuronal/glial cells

Bioorg Med Chem Lett. 2005 Jul 1;15(13):3220-3. doi: 10.1016/j.bmcl.2005.05.006.

Abstract

We have designed and synthesized several structural isomers of anthramycin (heterocycles 2, 3, 5, 6, and 8) and found that, in particular, pyrrolobenzodiazepine 8 induces DNA cleavage and formation of small fragments of DNA. The cytotoxic effects of 8 were manifested with both non-transformed primary neuronal/glial cells and transformed Jurkat cells. The other compounds did not change the viability either of transformed or of non-transformed cells, and induced DNA cleavage to a lesser extent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology
  • Benzodiazepines / chemical synthesis
  • Benzodiazepines / pharmacology*
  • Cell Survival / drug effects
  • Cells, Cultured
  • DNA / drug effects
  • DNA / metabolism
  • Humans
  • Jurkat Cells
  • Leukemia, T-Cell / drug therapy*
  • Leukemia, T-Cell / pathology
  • Neuroglia / drug effects*
  • Neurons / drug effects*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Benzodiazepines
  • DNA