Sulfonamide Derivatives of Benzylamine Block Cholesterol Biosynthesis in HepG 2 Cells: A New Type of Potent Squalene Epoxidase Inhibitors. -A new class of sulfonamide derivatives (VI) which act as mammalian squalene epoxidase inhibitors is synthesized. It is shown that thienyl residue is necessary
Trifluoromethyl ketones derived from squalene: inhibition of the cholesterol biosynthesis in HepG2 cells
✍ Scribed by Farid Benayoud; Ahmed Abouabdellah; Cyrille Richard; Danièle Bonnet-Delpon; Jean-Pierre Bégué; Danielle Levasseur; Olivier Boutaud; Francis Schuber
- Publisher
- Elsevier Science
- Year
- 2000
- Tongue
- French
- Weight
- 154 KB
- Volume
- 41
- Category
- Article
- ISSN
- 0040-4039
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✦ Synopsis
Tri¯uoromethyl ketones 1 and 2, have been prepared from trisnorsqualene aldehyde 3. These compounds and their corresponding alcohols 4 and 7 have been found to be good inhibitors of the biosynthesis of cholesterol in HepG2 cells. The inhibition is correlated with a decrease of the HMG-CoA reductase activity, probably resulting from the transformation of the ¯uorinated compounds into their corresponding oxysterols which could act as repressors of that enzyme.
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STUDIES on the enzymic synthesis of squalene from mevalonic acid (3:5dihydroxy-j-methylpentanoic acid) in yeast extracts have revealed a number of nei intermediates. 5-Phosphomevalonate,1'2'3 54iphosphomevalonate and 3-methylbut-J-en-l;yl. pyrophosphate (isopentenyl pyrophosphate) 4,5,6 have been re
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