Hydroxamates: Relationships between Structure and Plasma Stability | Zendy

Marion Flipo | Zendy; Julie Charton | Zendy; Akila Hocine | Zendy; Sandrine Dassonneville | Zendy; Benoît Déprez | Zendy; Rebecca DeprezPoulain | Zendy

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Hydroxamates: Relationships between Structure and Plasma Stability

Author(s) -

Marion Flipo,

Julie Charton,

Akila Hocine,

Sandrine Dassonneville,

Benoît Déprez,

Rebecca DeprezPoulain

Publication year - 2009

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm900648x

Subject(s) - chemistry , metabolic stability , vorinostat , combinatorial chemistry , stability (learning theory) , human plasma , chemical stability , drug discovery , pharmacology , computational biology , computational chemistry , stereochemistry , biochemistry , organic chemistry , machine learning , chromatography , histone deacetylase , computer science , in vitro , medicine , gene , histone , biology

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.

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