159554-45-7Relevant academic research and scientific papers
Sulfonamide derivatives of benzylamine block cholesterol biosynthesis in HepG2 cells: A new type of potent squalene epoxidase inhibitors
Gotteland,Loubat,Planty,Junquero,Delhon,Halazy
, p. 1337 - 1342 (1998)
Sulfonamide derivatives of ene-yne benzylamine 1 have been prepared and identified as a new class of potent SE inhibitors having demonstrated activity in HepG2 cells as cholesterol biosynthesis inhibitors.
Comparative study of new and known thienyl derivatives of ene-yne benzylamine as mammalian squalene epoxidase inhibitors
Gotteland,Junquero,Oms,Delhon,Halazy
, p. 333 - 342 (2007/10/03)
Analogs of the well-known squalene epoxidase inhibitor (SE) NB-598 (2) have been prepared and tested as cholesterol biosynthesis inhibitors in HepG2 cells. Among the compounds tested, the vinylthiophene analog 4 and the tertiary amide derivative of thiophene 8 emerged as potent human SE inhibitors and probably bind to the enzyme in a very similar manner as NB-598 (2). Surprisingly enough, compounds 4 and 8, contrary to NB-598, are poor inhibitors of rat SE, thus further demonstrating major differences between mammalian enzymes from different species.
