Cyclization-activated prodrugs. Basic esters of 5-bromo-2'-deoxyuridine

J Med Chem. 1990 Sep;33(9):2590-5. doi: 10.1021/jm00171a038.

Abstract

Some 3'- and 5'-[[(alkylamino)ethyl]glycyl] esters of 5-bromo-2'-deoxyuridine were prepared and evaluated in vitro as progenitors of the parent alcohol. The esters proved to be relatively stable at low pH but released 5-bromo-2'-deoxyuridine cleanly at rates which were pH and structure dependent. These basic esters are examples of cyclization-activated prodrugs in which generation of active drug is not linked to enzymatic cleavage but rather results from an intramolecular cyclization-elimination reaction.

MeSH terms

  • Bromodeoxyuridine / analogs & derivatives*
  • Chemical Phenomena
  • Chemistry
  • Cyclization
  • Esters
  • Prodrugs / chemical synthesis*
  • Prodrugs / pharmacokinetics
  • Structure-Activity Relationship

Substances

  • Esters
  • Prodrugs
  • Bromodeoxyuridine