Basic Information
ID: ALA1154615
Journal: J Med Chem
Title: Hydroxamates: relationships between structure and plasma stability.
Authors: Flipo M, Charton J, Hocine A, Dassonneville S, Deprez B, Deprez-Poulain R.
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.
CiteXplore: 19821586
DOI: 10.1021/jm900648x
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets