New topoisomerases inhibitors: synthesis of rutaecarpine derivatives and their inhibitory activity against topoisomerases

Arch Pharm Res. 2012 May;35(5):785-9. doi: 10.1007/s12272-012-0504-1. Epub 2012 May 29.

Abstract

A series of rutaecarpine derivatives were prepared by employing previously reported methods and their inhibitory activities against topoisomerase I and II were evaluated. Among them, strongly cytotoxic 10-bromorutaecarpine and 3-chlororutaecarpine showed strong inhibitory activities against topo I and II.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • DNA Topoisomerases, Type I / metabolism
  • DNA Topoisomerases, Type II / metabolism
  • Humans
  • Indole Alkaloids / chemical synthesis*
  • Indole Alkaloids / pharmacology
  • Quinazolines / chemical synthesis*
  • Quinazolines / pharmacology
  • Rutaceae*
  • Topoisomerase I Inhibitors / chemical synthesis*
  • Topoisomerase I Inhibitors / pharmacology
  • Topoisomerase II Inhibitors / chemical synthesis*
  • Topoisomerase II Inhibitors / pharmacology

Substances

  • Indole Alkaloids
  • Quinazolines
  • Topoisomerase I Inhibitors
  • Topoisomerase II Inhibitors
  • rutecarpine
  • DNA Topoisomerases, Type I
  • DNA Topoisomerases, Type II