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

ABSTRACT

The synthesis of ß-thiolactone and ß-lactam analogs of tetrahydrolipstatin is described from a common late-stage ß-lactone derivative. These analogs, and a cis-disubstituted ß-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.