Design, synthesis and evaluation of 4-imidazolylflavans as new leads for aromatase inhibition.
Two 4-imidazolylflavans were synthesized and their relative stereochemistry was established by 1H and 13C NMR data. These compounds were tested for their activity to inhibit aromatase. It was observed that the introduction of an imidazolyl group at carbon 4 on flavan nucleus led to potent molecules.
Pouget
Christelle
C
UPRES EA 1085, Biomolécules et cibles cellulaires tumorales, Faculté de Pharmacie, 2 rue du Docteur Marcland, Limoges, France.
Fagnere
Catherine
C
Basly
Jean-Philippe
JP
Habrioux
Gérard
G
Chulia
Albert Jośe
AJ
D001141:Aromatase / Q000737:chemistry; D047072:Aromatase Inhibitors; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D005419:Flavonoids / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D010920:Placenta / Q000201:enzymology; D011247:Pregnancy; D011522:Protons; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D047072:Aromatase Inhibitors; D004791:Enzyme Inhibitors; D005419:Flavonoids; D007093:Imidazoles; D011522:Protons; D001141:Aromatase