Article

Synthesis and biological investigation of the β-thiolactone and β-lactam analogs of tetrahydrolipstatin.

Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, CNRS, 1 Avenue de la Terrasse, 91190 Gif-sur-Yvette, France.
Organic & Biomolecular Chemistry (impact factor: 3.7). 04/2012; 10(13):2629-32. DOI:10.1039/c2ob06976h pp.2629-32
Source: PubMed

ABSTRACT The synthesis of β-thiolactone and β-lactam analogs of tetrahydrolipstatin is described from a common late-stage β-lactone derivative. These analogs, and a cis-disubstituted β-lactone analog of tetrahydrolipstatin, were screened for activity against porcine pancreatic lipase and for inhibition of cell growth of a panel of four human cancer lines.

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Keywords

analogs
 
cell growth
 
common late-stage β-lactone derivative
 
human cancer lines
 
inhibition
 
porcine pancreatic lipase
 
tetrahydrolipstatin
 
β-lactam analogs
 

Sylvain Aubry