(Aryloxy) methylsilane derivatives as new cholesterol biosynthesis inhibitors: synthesis and hypocholesterolemic activity of a new class of squalene epoxidase …
JP Gotteland, I Brunel, F Gendre, J Desire…
文献索引：Gotteland, Jean-Pierre; Brunel Isabelle; Gendre, Fabrice; Desire, Jerome; Delhon, Andre; at al. Journal of Medicinal Chemistry, 1995 , vol. 38, # 17 p. 3207 - 3216
A series of 3-substituted (ary1oxy) silane derivatives of benzylamine (4, 4, or 4) was synthetized and evaluated for hypocholesterolemic activity. Most of the new silane derivatives were identified as potent inhibitors of pig liver squalene epoxidase with IC50 values in the submicromolar range. In vitro inhibition of cholesterol biosynthesis in Hep-Gz cells was observed with a very good potency for the ene-yne derivatives 4a, 4i, 4n, 4q, ...
