SEARCH

SEARCH BY CITATION

Keywords:

  • angiogenesis;
  • anticancer agents;
  • camptothecin;
  • inhibitors;
  • topoisomerases

Abstract

The introduction of a methylenthiol group at position 7 of camptothecin was carried out in four steps. This preparation also yielded the corresponding disulfide, which behaves as a prodrug due to its reactivity with glutathione. Assessment of their antiproliferative activities, investigations of their mechanism of action, and molecular modeling analysis indicated that the 7-modified camptothecin derivatives described herein maintain the biological activity and drug–target interactions of the parent compound.