Hydroxamates: relationships between structure and plasma stability

J Med Chem. 2009 Nov 12;52(21):6790-802. doi: 10.1021/jm900648x.

Abstract

Hydroxamates are valuable tools for chemical biology as well as interesting leads for medicinal chemistry. Although many hydroxamates display nanomolar activities against metalloproteases, only three hydroxamates have reached the market, among which is the HDAC inhibitor vorinostat. Failures in development are generally attributed to lack of selectivity, toxicity, or poor stability. To help medicinal chemists with respect to plasma stability, we have performed the first and preliminary study on structure-plasma stability for hydroxamates. We define some structural rules to predict or improve the plasma stability in the preclinical stage.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Drug Evaluation, Preclinical
  • Drug Stability
  • Esterases / blood
  • Half-Life
  • Humans
  • Hydrolysis
  • Hydrophobic and Hydrophilic Interactions
  • Hydroxamic Acids / blood
  • Hydroxamic Acids / chemical synthesis*
  • Hydroxamic Acids / chemistry
  • Plasma
  • Prodrugs / chemical synthesis
  • Prodrugs / chemistry
  • Prodrugs / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Hydroxamic Acids
  • Prodrugs
  • Esterases