Stilbene analogs as inducers of apolipoprotein-I transcription

Based on the naturally occurring stilbene, Resveratrol, a series of novel stilbene derivatives were synthesized, which have the ability to induce the expression of the ApoA-I gene. Several compounds equally or more potent than Resveratrol were identified. trans-4,4′-Dihydroxy-2-methoxystilbene was t...

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Veröffentlicht in:	European journal of medicinal chemistry 2010-05, Vol.45 (5), p.2018-2023
Hauptverfasser:	Hansen, Henrik C., Chiacchia, Fabrizio S., Patel, Reena, Wong, Norman C.W., Khlebnikov, Vladimir, Jankowska, Renata, Patel, Kalpesh, Reddy, M. Madhava
Format:	Artikel
Sprache:	eng
Schlagworte:	Apolipoprotein A-I - genetics Apolipoprotein-I Atherosclerosis Biological and medical sciences Caco-2 Cells Cholesterol transport General and cellular metabolism. Vitamins High-density lipoprotein Humans Medical sciences Molecular Structure Pharmacology. Drug treatments Promoter Regions, Genetic - drug effects Promoter Regions, Genetic - genetics Stereoisomerism Stilbene derivatives Stilbenes - chemical synthesis Stilbenes - chemistry Stilbenes - pharmacology Structure-Activity Relationship Transcription Transcription, Genetic - drug effects Transcription, Genetic - genetics Up-Regulation - drug effects Up-Regulation - genetics
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Beschreibung
Zusammenfassung:	Based on the naturally occurring stilbene, Resveratrol, a series of novel stilbene derivatives were synthesized, which have the ability to induce the expression of the ApoA-I gene. Several compounds equally or more potent than Resveratrol were identified. trans-4,4′-Dihydroxy-2-methoxystilbene was the most potent (4.6× more potent than Resveratrol). These compounds provide an early lead into new drugs to treat atherosclerosis. [Display omitted]
ISSN:	0223-5234 1768-3254
DOI:	10.1016/j.ejmech.2009.12.076